TW200917962A - Pyrazole compounds for controlling invertebrate pests - Google Patents

Pyrazole compounds for controlling invertebrate pests Download PDF

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Publication number
TW200917962A
TW200917962A TW097132567A TW97132567A TW200917962A TW 200917962 A TW200917962 A TW 200917962A TW 097132567 A TW097132567 A TW 097132567A TW 97132567 A TW97132567 A TW 97132567A TW 200917962 A TW200917962 A TW 200917962A
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Taiwan
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group
alkyl
hydrogen
formula
compound
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TW097132567A
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Chinese (zh)
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Steffen Gross
Delphine Breuninger
Henricus Maria Martinus Bastiaans
Deyn Wolfgang Von
Michael Puhl
Karsten Koerber
Douglas D Anspaugh
Deborah L Culbertson
Hassan Oloumi-Sadeghi
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Basf Se
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    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/64Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/561,2-Diazoles; Hydrogenated 1,2-diazoles
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/64Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
    • A01N43/7071,2,3- or 1,2,4-triazines; Hydrogenated 1,2,3- or 1,2,4-triazines
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/74Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,3
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N47/00Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
    • A01N47/08Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having one or more single bonds to nitrogen atoms
    • A01N47/10Carbamic acid derivatives, i.e. containing the group —O—CO—N<; Thio analogues thereof
    • A01N47/18Carbamic acid derivatives, i.e. containing the group —O—CO—N<; Thio analogues thereof containing a —O—CO—N< group, or a thio analogue thereof, directly attached to a heterocyclic or cycloaliphatic ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/14Ectoparasiticides, e.g. scabicides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

The present invention relates to novel pyrazole compounds of the formulae I and II, to their salts and their N-oxides which can be used for combating or controlling invertebrate pests, in particular arthropod pests. The invention also relates to a method for controlling invertebrate pests by using these compounds. The present invention also relates to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a pyrazole radical of the formulae A1, A2 or A3 ♯ denotes the binding site to the remainder of formulae I or II; X1 is S, O or NR1a; X2 is OR2a, NR2bR2c, S(O)mR2d; X3 is a lone pair or oxygen; R1, R2 and R3 are, inter alia, hydrogen, and wherein R41, R42, R43, R51, R52, R53, R61, R62, R63, are as defined in claim 1.

Description

200917962 九、發明說明: 【發明所屬之技術領域】 一本發明係關於新n坐化合物,其可用於抵抗或控制無 脊椎害蟲,尤其節肢動物害蟲。本發明亦係關於藉由使用 該等化合物控制無脊椎害蟲之方法。本發明亦係關於包含 6亥等化合物之種子及農業及獸醫學組合物。 【先前技術】 …、脊椎害蟲且尤其節肢動物及線蟲會毀壞生長中及已收 Γ獲之農作物並侵襲木製房屋及商業建築物,從而造成食物 供應及財產之重大經濟損失。儘管已知大量殺蟲劑,但由 於靶害蟲能對該等試劑產生抗性,故持續需要抵抗諸如昆 蟲、蜘蛛及線蟲等節肢動物害蟲之新試劑。因此,本發明 目的係提供具有優良殺蟲活性並針對諸多不同無脊椎害蟲 (尤其針對難於控制之見蟲、蜘蛛及線蟲)顯示廣譜活性之 化合物。 WO 2 003/106427闡述吡唑羧酸之N-芳基醯胺,其中吡唑 I 環在甲醯胺基團之鄰位上具有2_吡啶基。其中提及化合物 可用於抵抗無脊椎害蟲。 WO 2004/046129闡述經2-(1-芳基吡唑_5_基)羰基胺基取 代之苯甲醯胺化合物,其中提及其可用於抵抗無脊椎害 蟲。 曰本專利第2007-77106號闡述1-(3_氣吡啶-2-基)-吡唑_5_ 基甲酸之N-芳基醯胺,其中提及其可用於抵抗無脊椎害 蟲。 133661.doc 200917962 中國專利第】92?8 r t m t.i ^ - 號聞述可用作農業化學殺細菌劑及 权真鹵劑之芳香族及雜 困μ夂 【發明内容】 w比咬基甲醯胺。 本^明目的係提供且有彳I _ _ &amp; &amp; &amp; 〃、有優良杈蟲活性(尤其殺昆蟲活性、 並針對諸多不同I脊始室&amp; …、介椎害蟲(尤其針對難於控制之昆蟲、 蜘蛛及線蟲)顯示廣譜活性之化合物。 已發現該等目的可拉士丁今&gt; S由下文式I及π化合物及其鹽(尤其 〆. 其辰業上或獸醫學上可接受之鹽)來達成。 在第一態樣中,本發明係關於控制無脊椎害蟲之方法, 該方法包含用殺蟲有效量之式⑷!吡唑化合物或其鹽或N· 氧化物處理害蟲、其食物供應、其棲息地或其繁殖地、或 其中生長或可生長害蟲之植物、種子、土壤、區域、材料 或環境、或欲防止受到害蟲侵襲或侵擾之材料、植物、種 子、土壤、表面或空間:200917962 IX. INSTRUCTIONS: [Technical field to which the invention pertains] One invention relates to a novel n-sitting compound which can be used to resist or control invertebrate pests, particularly arthropod pests. The invention also relates to a method of controlling an invertebrate pest by using such compounds. The invention is also directed to seeds and agricultural and veterinary compositions comprising compounds such as 6H. [Prior Art] ..., spinal insects and especially arthropods and nematodes can destroy growing and harvested crops and invade wooden houses and commercial buildings, resulting in significant economic losses in food supply and property. Although a large number of insecticides are known, since target pests are resistant to such agents, there is a continuing need for new agents that are resistant to arthropod pests such as insects, spiders, and nematodes. Accordingly, it is an object of the present invention to provide compounds which exhibit excellent insecticidal activity and which exhibit a broad spectrum of activity against a number of different invertebrate pests, especially against difficult to control insects, spiders and nematodes. WO 2 003/106427 describes N-aryl decylamines of pyrazole carboxylic acids in which the pyrazole I ring has a 2-pyridyl group at the ortho position of the formamide group. The compounds mentioned therein can be used to combat invertebrate pests. WO 2004/046129 describes benzamidine compounds substituted with 2-(1-arylpyrazol-5-yl)carbonylamino groups, which are mentioned for their use against invertebrate pests.曰 Patent No. 2007-77106 describes N-aryl decylamine of 1-(3-hydropyridin-2-yl)-pyrazole-5-carboxylic acid, which is mentioned as being useful for combating invertebrate pests. 133661.doc 200917962 Chinese Patent No. 92?8 rtm ti ^ - No. described as an agrochemical bactericide and a true halogen agent for aromatic and heterozygous μ夂 [Summary] w than bitten formazan . The purpose of this is to provide and have 彳I _ _ &amp;&amp;&amp; amp, have excellent aphid activity (especially insecticidal activity, and for many different I ridges &amp; ..., vertebrate pests (especially for difficult Controlled insects, arachnids, and nematodes) exhibit broad-spectrum activity of compounds. It has been found that these purposes can be obtained from the following formula I and π compounds and their salts (especially 其. their primordial or veterinary In a first aspect, the invention relates to a method of controlling an invertebrate pest, the method comprising treating with an insecticidally effective amount of a compound of the formula (4)! pyrazole compound or a salt thereof or an N·oxide Pests, their food supply, their habitat or their breeding grounds, or plants, seeds, soils, areas, materials or environments in which they grow or grow pests, or materials, plants, seeds, soils that are intended to be protected from pest infestation or infestation , surface or space:

Α 係式Al、A2或A3吡唑基Α Al, A2 or A3 pyrazolyl

A1 A2A1 A2

133661.doc 200917962 # 表示與式I或II之其餘部分之結合位點; X1 係 s、Q 或 NR_la ; X 係 OR2a、NR2bR2c、s(0)mR2d ; X3係孤電子對或氧; R1係氫、CN、(:]-(:〗〇-烷基、CVCw鹵代烷基、C3_Ci〇、 環烧基、C3-C10-齒代環烷基、C3-C10-環烷基甲基、 c3-c10-鹵代環烷基甲基、C2_Cl(r烯基、c2_Cl〇_鹵代 烯基、C2-C10-炔基、c3_c10-鹵代炔基、Cl-C4-伸境 基-CN、〇Ra、Cl_c4-伸烧基 _0Ra、c(Y)Rb、Ci_c4_伸 烷基-C(Y)Rb、C(Y)0Re、Cl_C4_ 伸烷基 _c(Y)〇RC、 S(〇)2Rd、NReRf、C1-C4-伸烧基-NReRf、c(Y)NRgRh、 CrC4-伸烧基-C(Y)NRgRh、S(0)mNReRf、C(Y)NRiNReRf、 苯基、雜芳基、苯基-cvcv烷基及雜芳基_Cl_c4_境 基,其中上述最後四個基團之芳香環可未經取代或可 具有1、2、3、4或5個相同或不同取代基Rx ; R 係氫、鹵素、Cl_C4_烷基、C〗-C4-鹵代烷基、(:,-(:4-¾ 氧基、(VC4-鹵代烷氧基、Cl_c4_烷硫基、Ci_c4_鹵代 烷硫基、CrC4-烷基亞磺醯基、Ci_c4_鹵代烷基亞磺 醯基、q-C4-烷基磺醯基、Ci_c4_鹵代烷基磺醯基、 c3-c6-環烧基、C3-C6-iS代環烧基、C2_C4_稀基、c2_ C4-鹵代烯基、C2-C4-炔基或Ci_c4_烷氧基 基; R3係氫、鹵素、G-cu-烷基、Ci_C4_鹵代烷基、Ci_C4_烷 氧基' CVC4-鹵代烷氧基、Ci_c4_烷硫基、Ci_c4_鹵代 133661.doc •9· 200917962 烧硫基、Cl々烧基亞石黃醯基、Ci_C4_齒代院基亞罐 醯基、c,々烧基項醯基、齒代烧基續酸基、133661.doc 200917962 # indicates a binding site to the rest of formula I or II; X1 is s, Q or NR_la; X is OR2a, NR2bR2c, s(0)mR2d; X3 isphaned electron pair or oxygen; R1 is hydrogen , CN, (:]-(: 〇-alkyl, CVCw haloalkyl, C3_Ci〇, cycloalkyl, C3-C10-dentocycloalkyl, C3-C10-cycloalkylmethyl, c3-c10- Halogenated cycloalkylmethyl, C2_Cl (r alkenyl, c2_Cl〇_haloalkenyl, C2-C10-alkynyl, c3_c10-haloalkynyl, Cl-C4-extension-CN, 〇Ra, Cl_c4 - Stretching base_0Ra, c(Y)Rb, Ci_c4_alkylene-C(Y)Rb, C(Y)0Re, Cl_C4_alkylene group _c(Y)〇RC, S(〇)2Rd, NReRf , C1-C4-alkylene-NReRf, c(Y)NRgRh, CrC4-alkylene-C(Y)NRgRh, S(0)mNReRf, C(Y)NRiNReRf, phenyl, heteroaryl, phenyl -cvcvalkyl and heteroaryl_Cl_c4_, wherein the aromatic ring of the last four groups described above may be unsubstituted or may have 1, 2, 3, 4 or 5 identical or different substituents Rx; Hydrogen, halogen, Cl_C4_alkyl, C--C4-haloalkyl, (:,-(:4-3⁄4 oxy, (VC4-haloalkoxy, Cl_c4_alkylthio, Ci_c4_haloalkylthio, CrC4- Alkyl Sulfhydryl, Ci_c4_haloalkylsulfinylene, q-C4-alkylsulfonyl, Ci_c4_haloalkylsulfonyl, c3-c6-cycloalkyl, C3-C6-iS cycloalkyl, C2_C4_ Dilute, c2_C4-haloalkenyl, C2-C4-alkynyl or Ci_c4_alkoxy; R3 is hydrogen, halogen, G-cu-alkyl, Ci_C4_haloalkyl, Ci_C4_alkoxy' CVC4 -haloalkoxy, Ci_c4_alkylthio, Ci_c4_halogen 133661.doc •9· 200917962 Sulphur-based, Cl-pyrene-based sulphate, Ci_C4_ 齿代院基亚罐醯基, c, 々烧基Xanthyl group, tooth-based alkyl group, acid group,

c3-c6-環院基、c3_c6· _代環燒基、Q々稀基、G ca代烯基、C2_C4_块基或Ci々烧氧基_Ci々院 基; 係〇、1或2 ;C3-c6-rings, c3_c6· _cycloalkyl, Q々 dilute, G ca alkenyl, C 2 —C 4 —block or Ci® alkoxy _Ci 々 基 ; ; ; ; ; ; ; ; ; ;

R 41 f R51 、R42、R43係選自由以下組成之群:氫、齒素、⑶、 叫、叫院基、^環貌基、^環稀基、 c3m基甲基、C2_Ci〇_烯基、c2_ci。·块基,盆 中上述最後6個基團之脂肪族或環狀部分可未經取 代、可經部分或完全“或可具有卜2或3個相同或 不同取代基 V、0Ra、SRa、c(Y)Rb、c⑺〇rc、 S ⑼#、NReRf、C(Y)NRgRh、笨基、苯基 _c 丨院 基本氧基-CVCV院基、5員雜芳基及雜環 基’其中上述最後5個基團之雜環基及芳香族環可未 經取代或可具有^小…個相同或不同取代基 Rx ; 系、自由以下組成之群:氫、鹵素、⑶、N〇2、 C,°_院基、環貌基、c5-c10-環稀基、c3_Cl。-環 烧基甲基、c2-Cl。-稀基、C2々。·炔基,其中上述最後 6個一基團之脂肪族或環狀部分可未經取代、可經部分 ,王鹵化或可具有1、2或3個相同或不同取代基R 41 f R51 , R42 and R43 are selected from the group consisting of hydrogen, dentate, (3), nickname, phenyl group, ring group, c3m group methyl group, C2_Ci〇-alkenyl group, C2_ci. Block basis, the aliphatic or cyclic moiety of the last six groups described above may be unsubstituted, partially or completely "or may have 2 or 3 identical or different substituents V, 0Ra, SRa, c (Y) Rb, c (7) 〇 rc, S (9) #, NReRf, C (Y) NRgRh, stupid, phenyl _c 丨 基本 basic oxy-CVCV, 5-membered heteroaryl and heterocyclic The heterocyclic group and the aromatic ring of the last 5 groups may be unsubstituted or may have the same or different substituents Rx; a group of free radicals: hydrogen, halogen, (3), N〇2, C , °_院基, ring-form, c5-c10-ring dilute, c3_Cl.-cycloalkylmethyl, c2-Cl.-dilute, C2々.. alkynyl, wherein the last six one groups The aliphatic or cyclic moiety may be unsubstituted, may be partially moieved, or may have 1, 2 or 3 identical or different substituents.

Ry、〇Ra、SRa、c⑺Rb、c⑺〇Re、s⑼2Rd、 NReRf、C(Y)赚Rh、苯基、苯基基、苯氧 133661.doc •10- 200917962Ry, 〇Ra, SRa, c(7)Rb, c(7)〇Re, s(9)2Rd, NReRf, C(Y) earn Rh, phenyl, phenyl, phenoxy 133661.doc •10- 200917962

R 52R 52

基々C4·烧基、5員雜芳基及雜環-cvc4-烧基,其中 上述最後5個基團之雜環基及芳香族環可未經取代或 可具有1、2、3、4或5個相同或不同取代基RX ; •R53係選自由以下組成之群:氫、齒素、cn、n〇2、 CrC】。-烷基、C3-Cl。-環烷基、C5_C丨。·環烯基、 c10-環烷基甲基、C2_Cl。,基、c2_Ci。-炔基,其中上 述最後6個基團之脂肪族或環狀部分可未經取代、可 經部分或完全齒化或可具有1、2或3個相同或不同取 代基 、〇Ra、SRa、c(Y)Rb、c⑺〇RC、s(〇)2Rd、 NReRf、c⑺NR£Rh、雜環基、苯基、苯基-Cl-c4-烧 基、苯氧基-CrC4-烷基及雜環_Ci_c4_烷基其中上述 最後5個基團之雜環基及芳香族環可未經取代或可具 有1、2、3、4或5個相同或不同取代基rX ; R63係選自由以下組成之群:氫、N〇2、口&lt;1〇_烷 基、C3-C1()-環烧基、C5_Cl()_環烯基、CA。-環烧基 甲基、C2_C10-烯基、C2_C10-炔基,其中上述最後6個 基團之脂肪族或環狀部分可未經取代、可經部分或完 全齒化或可具有1、2或3個相同或不同取代基Ry、 ORa、SRa、C(Y)Rb、c⑺〇RC、s(〇)2Rd、NReRf、 C(Y)NRgR、S(0)mNReRf、(^(Y^R'NReRf、雜環基、 苯基、苯基烷基、苯氧*_C|_C4_烷基及雜環_ C! -(V烷基’其中雜環基及芳香族環所述最後5個基 團之可未經取代或可具有丨、2、3、4或5個相同或不 同取代基Rx ; I33661.doc 200917962 R係選自由以下組成之群:氫、N〇2、Ci_c】〇_烧基、^ c『環烷基' c”Cl。-環烯基、C3_Ci〇•環烷基甲基、 C2-C〗〇-晞基、C2_Cl〇_快基,其中上述最後_基團之 脂肪族或環狀部分可未經取代、可經部分或完全函化 或可具有1、2或3個相同或不同取代基Ry、〇Ra、 SRa、C(Y)Rb、c⑺〇Re、s(〇)2Rd、NReRf、c⑺皿^、 S(0)mNReRf、C(Y)NRiNReRf、苯基、笨基 CIA 烷 基、苯氧基_C^_C4_烷基、5員雜芳基及雜環_C丨烷 基,其中上述最後5個基團之雜環基及芳香族環可未 經取代或可具有i、2、3、4或5個相同或不同取代基 Rx ; Y 係Ο或S ;a C4·alkyl group, a 5-membered heteroaryl group and a heterocyclic-cvc4-alkyl group, wherein the heterocyclic group and the aromatic ring of the last five groups described above may be unsubstituted or may have 1, 2, 3, 4 Or 5 identical or different substituents RX; • R53 is selected from the group consisting of hydrogen, dentate, cn, n〇2, CrC]. - alkyl, C3-Cl. - cycloalkyl, C5_C丨. - cycloalkenyl, c10-cycloalkylmethyl, C2_Cl. , base, c2_Ci. Alkynyl, wherein the aliphatic or cyclic moiety of the last six of the above groups may be unsubstituted, partially or fully dentated or may have 1, 2 or 3 identical or different substituents, 〇Ra, SRa, c(Y)Rb, c(7)〇RC, s(〇)2Rd, NReRf, c(7)NR£Rh, heterocyclic group, phenyl group, phenyl-Cl-c4-alkyl group, phenoxy-CrC4-alkyl group and heterocyclic ring _Ci_c4_alkyl wherein the heterocyclic group and the aromatic ring of the last five groups described above may be unsubstituted or may have 1, 2, 3, 4 or 5 identical or different substituents rX; R63 is selected from the group consisting of Groups: hydrogen, N〇2, mouth &lt;1〇-alkyl, C3-C1()-cycloalkyl, C5_Cl()-cycloalkenyl, CA. a cycloalkylmethyl group, a C2_C10-alkenyl group, a C2_C10-alkynyl group, wherein the aliphatic or cyclic moiety of the last six groups described above may be unsubstituted, partially or fully toothed or may have 1, 2 or 3 identical or different substituents Ry, ORa, SRa, C(Y)Rb, c(7)〇RC, s(〇)2Rd, NReRf, C(Y)NRgR, S(0)mNReRf, (^(Y^R' NReRf, heterocyclyl, phenyl, phenylalkyl, phenoxy*_C|_C4_alkyl and heterocyclic _C!-(V alkyl' wherein the last 5 groups of the heterocyclic group and the aromatic ring It may be unsubstituted or may have 丨, 2, 3, 4 or 5 identical or different substituents Rx; I33661.doc 200917962 R is selected from the group consisting of hydrogen, N〇2, Ci_c] 〇_alkyl , ^ c "cycloalkyl 'c" Cl.-cycloalkenyl, C3_Ci〇•cycloalkylmethyl, C2-C〗 〇-fluorenyl, C2_Cl〇_ fast radical, wherein the last _ group of aliphatic Or the cyclic moiety may be unsubstituted, may be partially or completely functionalized or may have 1, 2 or 3 identical or different substituents Ry, 〇Ra, SRa, C(Y)Rb, c(7)〇Re, s(〇 2Rd, NReRf, c(7) dish^, S(0)mNReRf, C(Y)NRiNReRf, phenyl, stupid CIA alkyl, benzene a — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — — , 4 or 5 identical or different substituents Rx; Y system or S;

Rla係選自氫、CVGo-烷基、CrCV鹵代烷基、C3_C|〇_環 烧基、c3-Cl0-環烷基甲基、c3_Ci0_鹵代環烷基、c2_ c10-烯基、C2-C10-i 代烯基、c2-c10-炔基、Cl_Cl〇-烷 氧基-C1-C4-烧基、〇Ra、苯基、雜芳基、苯基_cnc4_ 烧基及雜芳基-CfC:4-烧基,其中上述最後4個基團之 芳香族環可未經取代或可具有1、2、3、4或5個彼此 獨立地選自由以下組成之群之取代基:_素、氰基、 硝基、q-C4-烷基、cvcv鹵代烷基、cvcv烷氧基及 Ci-C4-鹵代烧氧基; R2a係選自CrCV烷基、C〗-C4-鹵代烷基、C3-C6-環烷基、 C3-CV _代環烷基、c2_c4_烯基、c2-C4- _代烯基、 c2-c4-炔基、Cl_c4_烷氧基_Cl_c4-烷基、苯基、雜芳 133661.doc 12 200917962 基、笨基-C^-C4-烷基及雜芳基_c〗_c4_烷基,其中上述 最後4個基團之芳香族環可未經取代或可具有丨、2、 3、4或5個彼此獨立地選自由以下組成之群之取代 基·鹵素、氰基、硝基、Cl_C4_烷基、Ci_C4_鹵代烷 基、CVC4·烷氧基及(^-(:4-鹵代烷氧基; R2b、R2e彼此獨立地選自氫、Ci_C4_烷基、Ci_c4_鹵代烷 基、C3-C6’烧基、C3-C6-鹵代環烷基、c2-C4-稀基、 c2-c4- _ 代烯基、c2-C4-块基、Cl_c4_烧氧基 _Ci_c4_ 烷基、C,-C4-烷基羰基、Ci_c4_鹵代烷基羰基、Ci_c4_ 烷基磺醯基、C^C4-鹵代烷基磺醯基、苯基、苯基羰 基、苯基磺醯基、雜芳基、雜芳基羰基、雜芳基磺醯 基、笨基-CrC4-烷基及雜芳基_Cl_c4_烷基,其中上述 最後8個基團中之芳香族環可未經取代或可具有1、 2、3、4或5個彼此獨立地選自由以下組成之群之取代 基:鹵素、氰基、硝基、Cl_C4_烷基、Ci_c4_ _代烷 基、C〗-C4-烷氧基及(^-(:4-鹵代烷氧基;或 R及R與其所鍵結之氮原子一起形成5_或6員飽和或不飽 和雜環’其可具有選自〇、5及N之另一雜原子作為環 成員原子且其中雜環可未經取代或可具有1、2、3、4 或5個彼此獨立地選自由以下組成之群之取代基:鹵 素、氰基、硝基、CVCV烷基、(VCV鹵代烷基、Cl_ Cr烷氧基及匚^匸^鹵代烷氧基; R2d係選自CVCV烷基、CVCV鹵代烷基、C3-C6-環烷基、 C3-c6- _代環烷基、C2_C4_烯基、C2_C4_鹵代烯基、 133661.doc -13- 200917962 c2 C4-块基、Cl_c4•貌氧基炫基、苯基、雜芳 基、苯基-CrC4-烷基及雜芳基_Ci_C4_烷基,其中上述 最後4個基團之芳香族環可未經取代或可具有1、2、 3、4或5個彼此獨立地選自由以下組成之群之取代 基.鹵素、氰基、硝基、Ci_c4_炫基、Ci_c4_ _代院 基、C^CV烷氧基及Cl_c4_鹵代烷氧基; R、R、Rc彼此獨立地選自氫、Ci_C4_烷基、鹵代 烷基、c3-c6-環烷基、c3_C6_環烷基甲基、C3_C6_鹵代 環烧基、C2-C4-稀基、c2-c4-鹵代稀基、C2-C4-快基、 C|-C4-院氧基_Cl_c4-院基、苯基、雜芳基、苯基_Ci_ C4_烧基及雜芳基_c「C4_烧基,其中上述最後4個基團 之芳香族環可未經取代或可具有丨、2、3、4或5個彼 此獨立地選自由以下組成之群之取代基:齒素、氰 基硝基' C1-C4 -院基、C!-C4-_代院基、C1-C4 -烧氧 基及C^-Cr鹵代烷氧基;Rla is selected from the group consisting of hydrogen, CVGo-alkyl, CrCV haloalkyl, C3_C|〇-cycloalkyl, c3-Cl0-cycloalkylmethyl, c3_Ci0_halocycloalkyl, c2_c10-alkenyl, C2-C10 -i alkenyl, c2-c10-alkynyl, Cl_Cl〇-alkoxy-C1-C4-alkyl, 〇Ra, phenyl, heteroaryl, phenyl_cnc4_alkyl and heteroaryl-CfC: a 4-alkyl group, wherein the aromatic ring of the last four groups described above may be unsubstituted or may have 1, 2, 3, 4 or 5 substituents independently of each other selected from the group consisting of: _, cyanide Base, nitro, q-C4-alkyl, cvcv haloalkyl, cvcv alkoxy and Ci-C4-haloalkoxy; R2a is selected from the group consisting of CrCV alkyl, C--C4-haloalkyl, C3-C6 -cycloalkyl, C3-CV-cycloalkyl, c2_c4-alkenyl, c2-C4-_alkenyl, c2-c4-alkynyl, Cl_c4_alkoxy_Cl_c4-alkyl, phenyl, hetero芳133661.doc 12 200917962, phenyl-C^-C4-alkyl and heteroaryl_c _c4_alkyl, wherein the aromatic ring of the last four groups described above may be unsubstituted or may have an antimony, 2. 3, 4 or 5 substituents independently selected from the group consisting of halogen, cyano, nitro, Cl_C4_alkyl, C i_C4_haloalkyl, CVC4·alkoxy and (^-(:4-haloalkoxy; R2b, R2e are independently selected from hydrogen, Ci_C4_alkyl, Ci_c4_haloalkyl, C3-C6' alkyl, C3 -C6-halogenated cycloalkyl, c2-C4-thinyl, c2-c4-_alkenyl, c2-C4-blockyl, Cl_c4_alkoxy-Ci_c4_alkyl, C,-C4-alkylcarbonyl , Ci_c4_haloalkylcarbonyl, Ci_c4_alkylsulfonyl, C^C4-haloalkylsulfonyl, phenyl, phenylcarbonyl, phenylsulfonyl, heteroaryl, heteroarylcarbonyl, heteroarylsulfonate An anthracene, a styryl-CrC4-alkyl and a heteroaryl-Cl_c4-alkyl group, wherein the aromatic ring of the last 8 groups described above may be unsubstituted or may have 1, 2, 3, 4 or 5 each other Substituents independently selected from the group consisting of halogen, cyano, nitro, Cl_C4_alkyl, Ci_c4_ _alkyl, C-C4-alkoxy, and (^-(:4-haloalkoxy) Or R and R together with the nitrogen atom to which they are bonded form a 5- or 6-membered saturated or unsaturated heterocyclic ring' which may have another hetero atom selected from the group consisting of ruthenium, 5 and N as a ring member atom and wherein the heterocyclic ring may be Unsubstituted or can have 1, 2, 3, 4 or 5 separate from each other a substituent selected from the group consisting of halogen, cyano, nitro, CVCV alkyl, (VCV haloalkyl, Cl_Cr alkoxy, and haloalkoxy; R2d is selected from CVCV alkyl, CVCV haloalkyl, C3-C6-cycloalkyl, C3-c6- _cycloalkyl, C2_C4-alkenyl, C2_C4_haloalkenyl, 133661.doc -13- 200917962 c2 C4-blockyl, Cl_c4 Oxylenyl, phenyl, heteroaryl, phenyl-CrC4-alkyl and heteroaryl-Ci_C4_alkyl, wherein the aromatic ring of the last four groups described above may be unsubstituted or may have 1, 2 , 3, 4 or 5 substituents independently of each other selected from the group consisting of halogen, cyano, nitro, Ci_c4_Hyun, Ci_c4_ _ 院, C^CV alkoxy and Cl_c4_haloalkoxy R, R, Rc are independently of each other selected from the group consisting of hydrogen, Ci_C4_alkyl, haloalkyl, c3-c6-cycloalkyl, c3_C6_cycloalkylmethyl, C3_C6_halocycloalkyl, C2-C4- Dilute, c2-c4-halogenated, C2-C4-fast, C|-C4-homolyl_Cl_c4-homo, phenyl, heteroaryl, phenyl-Ci_C4_alkyl and hetero Aryl-c"C4_alkyl, wherein the aromatic ring of the last four groups mentioned above is Unsubstituted or may have an anthracene, 2, 3, 4 or 5 substituents independently of each other selected from the group consisting of dentate, cyanonitro 'C1-C4-hospital, C!-C4-_ Derivatives, C1-C4-alkoxy and C^-Cr haloalkoxy;

Rd係選自CrCV烷基、CrCV鹵代烷基、c3-c6-環院基、 C3-C6-環烷基曱基、c3-c6-鹵代環烷基、c2-c4-稀基、Rd is selected from the group consisting of CrCV alkyl, CrCV haloalkyl, c3-c6-ring, C3-C6-cycloalkylindolyl, c3-c6-halocycloalkyl, c2-c4-diyl,

CrCc齒代稀基、C2_C4-快基、C1-C4-院氧基—c】c 院基、苯基、雜芳基、苯基-CrCr烷基及雜芳基_c「CrCc dentate, C2_C4-fast, C1-C4-homolyl-c]c, phenyl, heteroaryl, phenyl-CrCr alkyl and heteroaryl _c"

Cc烷基,其中上述最後4個基團之芳香族環可未經取 代或可具有1、2、3、4或5個彼此獨立地選自由以下 &amp;成之群之取代基…、氰基、硝,基、c丨々、虎 基、cvc4-鹵代烷基、CVC4-烷氧基及(^-(:4-_代烧氧 基; 1 133661.doc -14- 200917962a Cc alkyl group, wherein the aromatic ring of the last four groups described above may be unsubstituted or may have 1, 2, 3, 4 or 5 substituents independently of each other selected from the group consisting of the following &amp; , nitrate, base, c丨々, tiger base, cvc4-haloalkyl, CVC4-alkoxy and (^-(: 4-_ alkoxy; 1 133661.doc -14- 200917962

Re、Rf彼此獨立地選自氫、Ci_c4_烷基、C〗_C4_ _代烷 基、q-cv環烷基、C3_C0_環烷基甲基、C3_C6_齒代環 烷基、C2-C4-稀基、c2-C4-函代烯基、c2_c4_块基、 CVC4-烧氧基必;·烧基、Ci_C44基幾基、C1_C4_ 鹵代烷基羰基、Cl-C4_烷基磺醯基、Ci_c4__代烷基 h 基、苯基、苯基羰基、苯基磺醯基、雜芳基、雜 芳基幾基、雜芳基續醯基、苯基Ace基及雜芳 基-C^-C4-烷基,其中上述最後8個基團中之芳香族環 可未經取代或可具有i、2、3、4或5個彼此獨立地選 自由以下組成之群之取代基:齒素、氰基、硝基、 cvc4-烧基、Cl_c4_鹵代烧基、Ci_c4i氧基及 鹵代烷氧基;或Re, Rf are independently of each other selected from the group consisting of hydrogen, Ci_c4_alkyl, C _C4_ _alkyl, q-cv cycloalkyl, C3_C0_cycloalkylmethyl, C3_C6_dental cycloalkyl, C2-C4- Dilute, c2-C4-equivalent alkenyl, c2_c4_block, CVC4-alkoxy; bake, Ci_C44 yl, C1_C4_haloalkylcarbonyl, Cl-C4_alkylsulfonyl, Ci_c4__ Alkenyl h group, phenyl, phenylcarbonyl, phenylsulfonyl, heteroaryl, heteroaryl, heteroaryl fluorenyl, phenyl Ace and heteroaryl-C^-C4- An alkyl group, wherein the aromatic ring in the last eight groups described above may be unsubstituted or may have i, 2, 3, 4 or 5 substituents independently of each other selected from the group consisting of dentate, cyano , nitro, cvc4-alkyl, Cl_c4_haloalkyl, Ci_c4ioxy and haloalkoxy; or

Rm%其所鍵結之氮原子一起形成5_或6員飽和或不飽和 雜環,其可具有選自〇、之另一雜原子作為環成 員原子且其中雜環可未經取代或可具有丨、2、3、*或 5個彼此獨立地選自由以下組成之群之取代基:鹵 素、氰基、確基、Cl-C4-烧基、Led代烧基、^ C4_院氧基及(^-〇:4-鹵代烧氧基; …、心此獨立地選自氫^-烧基^丨^代炫 基、c3-c6-環烷基、c3-c6_ii代環烷基、C2_C4_稀基、 c2-c4-幽代稀基、C2_C4_块基、Ci_c4_貌氧基 烷基、苯基、雜芳基、苯基_Ci_C4_烷基及雜芳基…广 Cc烷基,其中上述最後4個基團之芳香族環可^經取_ 代或可具有1、2、3、4或5個彼此獨立地選自由以下 133661.doc •15- 200917962 鹵素 '氰基、硝基、Ci_C4_烷 Cl-cv烷氧基及&lt;^-0:4-鹵代烷氧 係選自由以下組成之群:氣、Ci々院基、d々齒 ㈣、㈣-環院基、C3_C6姻基甲基、 代環烧基、CVCV烯基、c2_C4•由代烯基、C2_C41 基、cvcv院氧基-cvc4_烧基、苯基及苯基-燒 基,其中上述最後2個基團中之苯環可未經取代或可 V、有1 2 3 4或5個彼此獨立地選自由以下組成之 群之取代基··画素、氰基、硝基、Ci_C4基、 (V幽代烷基、cvcv烷氧基及^^广齒代烷氧基; 係選自由以下組成之群:鹵素、氰基、硝基、Ci_c4_ 烷基、CVC4-鹵代烷基、C|_C4_烷氧基、Ci_c4_鹵代烷 氧基、硫基、Ci_c4_鹵代烷硫基、Ci_c4_烷基 亞績醯基、CrC4-鹵代烷基亞磺醯基、Cl_c4_烷基磺 \ 組成之群之取代基 基、CVCV鹵代烷基 基; R(Rm% together with the nitrogen atom to which they are bonded form a 5- or 6-membered saturated or unsaturated heterocyclic ring which may have another hetero atom selected from fluorene as a ring member atom and wherein the heterocyclic ring may be unsubstituted or may have丨, 2, 3, * or 5 substituents independently of each other selected from the group consisting of halogen, cyano, decyl, Cl-C4-alkyl, Led alkyl, ^C4_houseoxy and (^-〇: 4-halogenated alkoxy; ..., the core is independently selected from the group consisting of hydrogen^-alkyl group, cyclyl, c3-c6-cycloalkyl, c3-c6_ii cycloalkyl, C2_C4 _ dilute, c2-c4-periodic, C2_C4_block, Ci_c4_morphyloxyalkyl, phenyl, heteroaryl, phenyl-Ci_C4_alkyl and heteroaryl... wide Cc alkyl, The aromatic ring of the above four last groups may be taken or may have 1, 2, 3, 4 or 5 independently of each other selected from the following 133661.doc •15- 200917962 halogen 'cyano, nitro The Ci_C4_alkane Cl-cv alkoxy group and the &lt;^-0:4-haloalkoxy group are selected from the group consisting of: gas, Ci 々 院, d々 (4), (4)-ring, and C3_C6. Methyl, cycloalkyl, CVCV alkenyl, c2_C4 • by alkenyl, C2_C41 a compound, a cvcv-oxyl-cvc4-alkyl group, a phenyl group and a phenyl-alkyl group, wherein the benzene ring in the last two groups may be unsubstituted or may be V, have 1 2 3 4 or 5 independent of each other. a substituent selected from the group consisting of a cyano group, a cyano group, a nitro group, a Ci_C4 group, a (V oxiranyl group, a cvcv alkoxy group, and a koji alkoxy group); Group: halogen, cyano, nitro, Ci_c4_alkyl, CVC4-haloalkyl, C|_C4_alkoxy, Ci_c4_haloalkoxy, thio, Ci_c4_haloalkylthio, Ci_c4_alkyl sulfhydryl , CrC4-haloalkylsulfinyl, Cl_c4_alkylsulfonate, a substituent group of the group, CVCV haloalkyl; R (

Rx 酿基、Ci-CV^代烷基磺醯基、Cl-C4-烷基羰基、CV cv鹵代烧基羰基、c3_c6_環烷基' c3_c6_鹵代環烷 基、C2-C4-烯基、c2-C4- _代烯基、C2-C4-炔基及C,-C4-烧氧基- C〗-C4-絶基;Rx Brewing, Ci-CV^alkylsulfonyl, Cl-C4-alkylcarbonyl, CV cv haloalkylcarbonyl, c3_c6_cycloalkyl' c3_c6_halocycloalkyl, C2-C4-ene a group, a C2-C4-_alkenyl group, a C2-C4-alkynyl group, and a C,-C4-alkoxy group-C--C4-based group;

Ry 彼此獨立地選自CrCc烷基、CrCcii代烷基、C〗-C4-烧氧基、Ci-C4·鹵代烧氧基、C1-C4-炫硫基、Ci-C4-鹵 代院硫基、CVC4-烧基亞橫醯基、cvCri代院基亞 績醯基、CVC4-垸基績醯基、C1-C4-鹵代烧基確醯 基、C3-C6-環燒基、C3-C6-鹵代環悅基、CrCr稀基、 13366l.doc -16- 200917962 c2-c4-鹵代烯基、 ^ ^ 2-c4-炔基、Ci_C4_烧氧基 _Ci_C4_ 烧基及CVC^-烷基羰基。 古t第二態樣中’本發明提供控制無脊椎害蟲之方法,該 ㈣蟲有效量之式1或叫嗤化合物或其鹽或祕 匕物或用权蠢有欵量之含右δ小 ^ 、 3有至^ ~種式I或II吡唑化合物或 鹽或Ν-氧化物之農紫έ日八札杏 &amp; έ 、 晨業、、且合物處理害蟲、其食物供應、其 棲心地或其繁殖地、哎盆中 + 次具中生長或可生長害蟲之植物、植 物繁殖材料(例如種子) 裡于)土壌、區域、材料或環境、或欲 防止受到害蟲侵襲或侵播 (ι Λ u擾之材枓、植物、植物繁殖材料 (例如種子)、土壤、表面或空間。 在第三態樣中’本發明提供針對無脊椎害蟲之侵擾保護 Π及/或自其生長之植物之方法,該方法包含用殺蟲有 ’里之式I或II化合物或其農業上可接受之鹽或 理種子。本發明另一目的 处Ry is independently selected from the group consisting of CrCc alkyl, CrCcii alkyl, C-C4-alkoxy, Ci-C4. halo-oxyloxy, C1-C4-thiol, Ci-C4-halogen Base, CVC4-alkyl sulphide, cvCri 代基基基醯, CVC4-垸基醯 base, C1-C4-haloalkyl thiol, C3-C6-cycloalkyl, C3- C6-halocyclohexyl, CrCr dilute, 13366l.doc -16- 200917962 c2-c4-haloalkenyl, ^^2-c4-alkynyl, Ci_C4_alkoxy-Ci_C4_ alkyl and CVC^- Alkylcarbonyl. In the second aspect of the ancient t, the present invention provides a method for controlling an invertebrate pest, and the effective amount of the formula (1) is called 嗤 compound or its salt or secret substance or the right δ is small. , 3~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~ Or plants in their breeding grounds, in pots, or in plants that grow or grow pests, plant propagation materials (such as seeds), in soil, areas, materials, or environments, or to prevent pests from invading or invading (ι Λ a material, a plant, a plant propagation material (such as a seed), a soil, a surface or a space. In a third aspect, the invention provides a method for infesting and protecting a plant from which an invertebrate pest infests The method comprises the use of a compound of formula I or II or an agriculturally acceptable salt or physiochemical seed thereof.

的係種子’其包含至少-種式1或II 化a物及/或其農業上可接受之鹽或义氧化物。 /發W外提供處理或保護動物以抵抗寄生蟲侵擾或感 木之方法’其包含使動物與殺寄生蟲有效量之如上文所定 義之式I或II化合物或其獸醫學上可接受之鹽或N_氧化㈣ 觸。使動物與本發明化合物1或Π、其鹽或獸醫學組合物接 觸意指將其施用或投與至動物。 迄今為止’仍未闡述式!別化合物及其鹽,但 合以下條件之式I化合物 付 -A具有式Α2,Χι係〇,Rl、r2、r3、r42及^各自為 風’且R53係2-經基苯基、2_經基_5_f基苯基、2_經基- I33661.doc 200917962 5-乙基苯基、2-羥基-5-氣笨基、2_羥基_45_二甲基苯 基、2-羥基-3,4-二甲基苯基或2_羥基_3,5_二甲基笨 基, -A具有式A3,X1係〇,、r2、r3、r43及r63各自為 氫,且R53係苯基、4-氟笨基、4_甲氧基苯基、4_溴苯 基、4-氯苯基、4-曱基苯基、4_乙氧基苯基、2,4_二甲 基苯基、2-羥基苯基、2-羥基_5_甲基苯基、2_羥基-% 乙基苯基、2-羥基-5-氣笨基、2_羥基_4,5_二甲基苯 基、2-羥基-3,4-二甲基笨基或2_羥基_3,5_二甲基笨 基, _ X係Ο,R ' R及R3各自為氣且八係W苯基甲基㈠-硝 基吡唑-5-基、丨_甲基吡唑巧_基、丨_甲基_4_氣吡唑·5_ 基、1-乙基-4-溴吡唑-3-基、i_乙基_3_曱基吡唑_4基、 1-甲基-3-三氟甲基吡唑_4_基、丨_苯基_5_苯甲醯基胺基 吡唑-4-基、l_(4-氣苯基)_3_苯基胺基羰基_5_甲基吡唑_ 4-基、1-苯基_5-[(4-曱基苯基)羰基]胺基吡唑·4_基、4_ 碘吡唑·3-基、1 -甲基吡唑-3-基、5-氣-1 -甲基吡唑_3_ 基、5-硝基吧唑_3_基、ι·(4_氯苯基)_5_三氟曱基11比唑_ 4-基、1-苯基_3_嗔吩-2-基&quot;比&quot;坐-4-基、1-苯基_3,5-二甲 基吡唑-4-基、4-溴-5-硝基吡唑-3-基或5-環丙基-ΐ-(ι,ι_ 二氧代四氫噻吩_3_基)-!H-吡唑-3-基; 且以下化合物除外: -1-(4-氯本基)-5-三氟甲基-比。坐-4-曱酸吼σ定-3-基醯 胺, 133661.doc -18- 200917962 -丨-苯基-3-噻吩_2_基-1H-吡唑-4-曱酸吡啶-3-基醯胺, 3’5 —甲基-1-苯基坐-4-甲酸吼咬-3-基酿胺。 因此’本發明亦包含式I及II新穎吡唑化合物及其鹽,具 體而言其農業上或獸醫學上可接受之鹽、及其Ν-氧化物。 本發明另一目的係農業組合物,其含有至少—種如上文 所疋義之新穎式I或II。比。坐化合物及/或其農業上可接受之 鹽或Ν-氧化物及至少一種液體或固體載劑。 本發明另一目的係獸醫學組合物,其含有至少一種如上 文所定義之新穎式I或II吡唑化合物及/或其獸醫學上可接 受之鹽或Ν-氧化物及至少一種獸醫學上可接受之液體或固 體載劑。 本發明另外係關於諸如種子等植物繁殖材料,其包含至 少一種本文所定義之式I或II化合物。 本發明另外係關於本文所定義式1或U化合物控制無脊椎 害蟲之用途。 【實施方式】 在式I或II化合物中,在八或。比啶基環上之取代基可含有 一或多個手性中心。在此情況下,端視取代基,式 合物可以不同對映異構體或非對映異構體形式存在。在式 Π情況下’化合物„亦可參照N=c軸以順式-或反式·異構體 形式存在。本發明係關於通式丨或^化合物之每一可能立體 異構體,即係關於單—對映異構體或非對映異構體以及其 混合物。 式I或II化合物可為非晶形或可以—或多種不同晶體狀態 133661.doc -19- 200917962 (多晶型)存在,其可具有諸如穩定性等不同宏觀特性或顯 示諸如活性等不同生物學特性。 本發明包括非晶形及晶體式〗或π化合物二者、化合物^ 或II各自不同晶體狀禮之混合物、以及其非晶形或晶體 鹽。 式I或Π化合物之鹽較佳為農業上及獸醫學上可接受之 鹽。其可以習知方法來形成,例如若式I化合物具有鹼性 B月b團則可藉由使化合物與所述陰離子之酸反應來形成, 或藉由使式I或Π酸性化合物與適宜鹼反應來形成。 化合物I及II之農業上可用之鹽尤其涵蓋彼等陽離子之鹽 或彼等酸之酸加成鹽’其各自之陽離子及陰離子對化合物 I或II之殺蟲作用無不利影響。因此適宜陽離子具體而古係 驗金屬(鈉及斜較佳)離子 '驗土金屬(約、鎂及鋇較佳)離 子、過渡金屬(錳、銅、鋅及鐵較佳)離子,亦及銨離子, 其若需要可具有一至四個C1々烷基取代基及/或一個苯基 或苄基取代基(二異丙基銨、四甲基銨四丁基銨、三曱 基节基錢較佳)’以及鱗離子、疏離子(三((VCV絲)疏較 佳)及氧化錡離子(三(C丨-C4·烷基)氧化巯較佳)。 可用酸加成鹽之陰離子主要係氯離子、漠離子、氣離 子、硫酸氫根離子、硫酸根離子H氫根離子、填酸 氫根離子、磷酸根離子、硝酸根離子、碳酸氫根離子、碳 酸根離子、六氟石夕酸根離子、六氣填酸根離子、苯甲酸根 離子及CrC4-鏈烷酸(較佳為曱酸鹽、乙酸鹽、两酸鹽及丁 酸鹽)之陰離子。其可藉由使式⑷!化合物與對應陰離子 133661.doc -20- 200917962 之酸(較佳為鹽酸、氫溴酸、硫酸、構酸或硝酸)反應來形 成。 式(I)化合物之獸醫學上可接受之鹽尤其涵蓋業内已知或 已接受用於形成獸醫學用鹽之彼等陽離子之鹽或酸加成 鹽。適宜酸加成鹽(例如由含有諸如胺基等鹼性氮原子之 式I或II化合物形成)包括與無機酸形成之鹽,例如鹽酸 鹽、硫酸鹽、磷酸鹽、及硝酸鹽;及有機酸之鹽,例如乙 酸、馬來酸(例如馬來酸之一元酸鹽或二元酸鹽)、二馬來 酸、富馬酸(例如富馬酸之一元酸鹽或二元酸鹽)、二富馬 酸、曱烷次磺酸、甲烷磺酸、及琥珀酸之鹽。 術語氧化物&quot;包括任何式化合物’除具有部分χ3 之吡啶氮之外,其具有至少一個氧化至沁氧化物部分之三 級亂原子。 涵蓋諸如昆蟲、蜘蛛及線蟲The seed of the invention comprises at least one of the formula 1 or II and/or an agriculturally acceptable salt or an antioxidant thereof. Providing a method of treating or protecting an animal against parasite infestation or sensation of wood - comprising an effective amount of an animal and a parasiticidal compound of formula I or II as defined above or a veterinary acceptable salt thereof Or N_oxidation (four) touch. Contacting an animal with a compound 1 or hydrazine, a salt thereof or a veterinary composition of the invention means administering or administering it to an animal. So far, it has not been elaborated! Other compounds and their salts, but the compound of formula I, which has the following conditions, has a formula of Α2, Χι system 〇, Rl, r2, r3, r42 and ^ are each of the wind' and R53 is 2-phenylidene, 2_经5_fylphenyl, 2_carbyl-I33661.doc 200917962 5-ethylphenyl, 2-hydroxy-5-indolyl, 2-hydroxy-45-dimethylphenyl, 2-hydroxy- 3,4-Dimethylphenyl or 2-hydroxyl-3,5-dimethylphenyl, -A has the formula A3, X1 is hydrazine, and r2, r3, r43 and r63 are each hydrogen, and R53 is benzene. Base, 4-fluorophenyl, 4-methoxyphenyl, 4-bromophenyl, 4-chlorophenyl, 4-nonylphenyl, 4-ethoxyphenyl, 2,4-dimethyl Phenyl, 2-hydroxyphenyl, 2-hydroxy-5-methylphenyl, 2-hydroxy-% ethylphenyl, 2-hydroxy-5-indolyl, 2-hydroxy- 4,5-dimethyl Phenylphenyl, 2-hydroxy-3,4-dimethylphenyl or 2-hydroxy-3,5-dimethylphenyl, _X Ο, R'R and R3 are each gas and octagonal W benzene Methyl(mono)-nitropyrazol-5-yl, 丨-methylpyrazole-5, 丨_methyl_4_apyrazol-5-yl, 1-ethyl-4-bromopyrazole-3 -yl, i_ethyl_3_mercaptopyrazole-4-yl, 1-methyl-3-trifluoromethylpyrazole-4-yl, 丨_phenyl_5_phenyl Merylaminopyrazol-4-yl, 1-(4-phenylphenyl)-3-phenylaminocarbonyl-5-methylpyrazole-4-yl, 1-phenyl-5-[(4-indole) Phenyl)carbonyl]aminopyrazole-4-yl, 4-iodopyrazol-3-yl, 1-methylpyrazol-3-yl, 5-a-1-1-methylpyrazole-3-yl, 5 -Nitrobazole _3_ group, ι·(4_chlorophenyl)_5_trifluoromethyl 11 azole -4-yl, 1-phenyl _3_ porphin-2-yl &quot; ratio &quot Sodium-4-yl, 1-phenyl-3,5-dimethylpyrazol-4-yl, 4-bromo-5-nitropyrazol-3-yl or 5-cyclopropyl-indole-( Ig,ι_dioxotetrahydrothiophene-3-yl)-!H-pyrazol-3-yl; and the following compounds are excluded: -1-(4-chlorobenzyl)-5-trifluoromethyl-ratio.曱-4-曱酸吼σ定-3-ylguanamine, 133661.doc -18- 200917962 -丨-phenyl-3-thiophene-2-yl-1H-pyrazole-4-furoic acid pyridine-3- Baseline amine, 3'5-methyl-1-phenyl-s--4-carboxylic acid bite-3-ylamine. Thus, the present invention also encompasses novel pyrazole compounds of the formulae I and II and salts thereof, in particular agriculturally or veterinary acceptable salts thereof, and their cerium-oxides. Another object of the invention is an agricultural composition comprising at least one novel Formula I or II as defined above. ratio. The compound and/or its agriculturally acceptable salt or cerium-oxide and at least one liquid or solid carrier are employed. Another object of the invention is a veterinary composition comprising at least one novel pyrazole compound of the formula I or II as defined above and/or a veterinary acceptable salt or cerium-oxide thereof and at least one veterinary Acceptable liquid or solid carrier. The invention further relates to plant propagation material, such as seeds, comprising at least one compound of formula I or II as defined herein. The invention further relates to the use of a compound of formula 1 or U as defined herein for controlling an invertebrate pest. [Examples] In the compound of formula I or II, it is in the eight or. Substituents on the pyridyl ring may contain one or more chiral centers. In this case, the terminal substituents, the formula may exist in different enantiomeric or diastereomeric forms. In the case of the formula, the 'compounds' may also be present in the cis- or trans-isomer form with reference to the N=c axis. The present invention relates to each possible stereoisomer of the formula 丨 or ^ compound, ie, With respect to mono-enantiomers or diastereomers and mixtures thereof. The compounds of formula I or II may be amorphous or may exist - or a plurality of different crystalline states 133661.doc -19- 200917962 (polymorph), It may have different macroscopic properties such as stability or exhibit different biological properties such as activity. The present invention includes a mixture of amorphous and crystalline or π compounds, compounds ^ or II, and a mixture of crystals, and Crystalline or crystalline salt. The salt of formula I or hydrazine compound is preferably an agriculturally and veterinary acceptable salt. It can be formed by conventional methods, for example, if the compound of formula I has a basic B group b The compound is formed by reacting the acid with the anion, or by reacting a compound of formula I or hydrazine with a suitable base. The agriculturally acceptable salts of compounds I and II specifically cover the salts of such cations or their acids. Acid plus The salt's respective cations and anions have no adverse effect on the insecticidal action of the compound I or II. Therefore, it is suitable for the specific cation and the ancient metal test (sodium and oblique preferred) ion soil test metal (about, magnesium and strontium are preferred). An ion, a transition metal (manganese, copper, zinc, and iron) ion, and an ammonium ion, which may have one to four C1 alkyl substituents and/or a phenyl or benzyl substituent, if desired. Isopropylammonium, tetramethylammonium tetrabutylammonium, triterpene basal acid is preferred) and scaly ions, sparse ions (three ((VCV filament) is preferred) and cerium oxide ions (three (C) -C4·alkyl) ruthenium oxide is preferred. The anion of the acid addition salt is mainly chloride ion, desert ion, gas ion, hydrogen sulfate ion, sulfate ion H hydrogen ion, acid hydrogen ion, phosphoric acid Root ion, nitrate ion, hydrogencarbonate ion, carbonate ion, hexafluoride ion, hexahydrate acid ion, benzoate ion and CrC4-alkanoic acid (preferably citrate, acetate, An anion of a two acid salt and a butyrate) which can be made by formula (4) Formed by reacting with an acid of the corresponding anion 133661.doc -20- 200917962 (preferably hydrochloric acid, hydrobromic acid, sulfuric acid, acid or nitric acid). Veterinarily acceptable salts of the compound of formula (I) are especially encompassed by the industry. Salts or acid addition salts of such cations which are known or accepted for the formation of veterinary salts. Suitable acid addition salts (for example formed from compounds of formula I or II containing a basic nitrogen atom such as an amine group) Including salts with inorganic acids, such as hydrochlorides, sulfates, phosphates, and nitrates; and salts of organic acids, such as acetic acid, maleic acid (eg, maleate or dibasic acid salt) a salt of dimaleic acid, fumaric acid (such as a monobasic acid salt or a dibasic acid salt of fumaric acid), difumaric acid, decane sulfenic acid, methanesulfonic acid, and succinic acid. The term oxide&quot; includes any compound of the formula&apos; having, in addition to the pyridinium nitrogen having a portion of χ3, having at least one disordered atom oxidized to the cerium oxide moiety. Covering insects, spiders and nematodes

或移植時或在此之 植物繁殖材料。 之前可用植物保護化合物 預防性處理該等 本文所用術語”無脊椎害蟲&quot;涵蓋諸 等動物種群’其可侵襲植物由此導致 損傷’以及外寄生蟲,其可侵擾諾士 I3366I.doc -21 · 200917962 本文所用術語”栽培植物,,包括已藉由繁殖、誘變或遺傳 工程改變之植物。經遺傳修飾之植物係如下植物:其遺傳 物質已藉由使用重組DNA技術來改變,其在天然環境下不 能由雜交育種、突變或天然重組獲得。通常,已將一或多 個基因整合至經遺傳修飾植物之遺傳物質中,以便改良該 植物之某些特性。該等遺傳修飾亦包括(但不限於)藉由(例 如)糖基化或聚合物加成(例如異戊二烯化、乙醯化或法呢 基化部分或PEG部分)實施之蛋白質(募-或多肽)聚合物之 乾向轉譯後修飾(例如以下文獻中所揭示:Biotechn〇1Or plant propagation material at the time of transplantation or here. Prophylactic treatment of plant protection compounds previously may be used herein. The term "invertebrate pests" encompasses animal populations that invade plants thereby causing damage and ectoparasites, which can invade Knots I3366I.doc -21 200917962 The term "cultivating plants" as used herein, includes plants that have been altered by propagation, mutagenesis or genetic engineering. Genetically modified plants are plants whose genetic material has been altered by the use of recombinant DNA techniques which are not obtainable by cross-breeding, mutation or natural recombination in the natural environment. Typically, one or more genes have been integrated into the genetic material of a genetically modified plant in order to modify certain characteristics of the plant. Such genetic modifications also include, but are not limited to, proteins implemented by, for example, glycosylation or polymer addition (eg, prenylation, acetamylation or farnesylation or PEG moieties) - or polypeptide) dry-to-translational modification of the polymer (eg as disclosed in the literature below: Biotechn〇1

Prog. 2001 年7_8 月;17⑷:72〇-8.,Pr〇tein ㈣ Des Sel· 2004 年 6 A;l7(l):57-66,Nat,Pr〇t〇C.2007;2(5):1225- 35.,Curr. 〇pin. Chem. Biol. 2006年 10 月;10(5):487_91 Epub 2006 年 8 月 28 曰,Biomaterials. 2001 年 3 月;22(5)· 405-17, BioconjugChem. 2005 年 1-2 月;16(1):113-21)。 本文所用術語”栽培植物&quot;另外包括藉由育種或遺傳工程 之習用方法已獲得對施用特定種類除草劑具有耐受力之植 物’該等除草劑為(例如)羥基-苯基丙酮酸雙加氧酶 (HPPD)抑制劑,乙醯乳酸合酶(alS)抑制劑,例如確醯脲 類(參見(例如)美國專利第6,222,100號、WO 01/82685、Prog. July 7/8, 2001; 17(4): 72〇-8., Pr〇tein (iv) Des Sel· 2004 6 A; l7(l): 57-66, Nat, Pr〇t〇C.2007; 2(5) :1225- 35., Curr. 〇pin. Chem. Biol. October 2006; 10(5): 487_91 Epub August 28, 2006 Bio, Biomaterials. March 2001; 22(5)· 405-17, BioconjugChem. January-February 2005; 16(1): 113-21). The term "cultivated plants" as used herein also includes plants which have been rendered tolerant to the application of a particular class of herbicides by conventional methods of breeding or genetic engineering. The herbicides are, for example, hydroxy-phenylpyruvate Oxygenase (HPPD) inhibitor, acetaminolate synthase (alS) inhibitor, for example, urinary urea (see, for example, U.S. Patent No. 6,222,100, WO 01/82685,

WO 00/26390、WO 97/41218、WO 98/02526、WO 98/02527、WO 04/106529、WO 05/20673、WO 03/14357、 WO 03/13225、WO 03/14356、WO 04/16073)或咪唑啉_ (參見(例如)美國專利第6,222,100號、WO 01/82685、WO 00/26390、WO 97/41218、WO 98/02526、WO 98/02527、 133661.doc •22· 200917962WO 00/26390, WO 97/41218, WO 98/02526, WO 98/02527, WO 04/106529, WO 05/20673, WO 03/14357, WO 03/13225, WO 03/14356, WO 04/16073) Or imidazoline _ (see, for example, U.S. Patent No. 6,222,100, WO 01/82685, WO 00/26390, WO 97/41218, WO 98/02526, WO 98/02527, 133661.doc • 22· 200917962

WO 04/106529、WO 05/20673、WO 03/14357、WO 03/13225、WO 03/143 56、WO 04/16073);烯醇丙 _ 醯莽 草酸-3-磷酸合酶(Epsps)抑制劑,例如草甘膦 (glyphosate)(參見(例如)WO 92/00377);谷胺醯胺合成酶 (GS)抑制劑,例如草錄膦(glufosinate)(參見(例如)歐洲專 利第 EP-A-0242236號、第 EP-A-242246號)或咢尼(oxynil) 除草劑。已藉由習用育種(誘變)方法賦予若干栽培植物對 除草劑之耐受性’例如Clearfield®小白菜(芸苔(Can〇la))對 咪唾琳酮(例如曱氧咪草煙)具有耐受性。已使用遺傳工程 方法來賦予栽培植物(例如大豆、棉花、玉米、甜菜及油 菜)對除草劑(例如草甘膦及草銨膦)之耐受性,其中某些除 草劑可以商品名RoundupReady®(草甘膦)及LibertyLink®(草 銨膦)購得。 本文所用術語”栽培植物”另外包括藉由使用重組DN a技 術而能合成以下產物之植物:一或多種殺昆蟲蛋白,尤其 已知來自細菌屬芽孢桿菌(bacillus)、具體而言來自蘇雲金 芽孢桿菌(bacillus thuringiensis)之彼等,例如a-内毒素, 例如 CrylA(b)、CrylA(c)、CrylF、CryIF(a2)、CryllA(b)、WO 04/106529, WO 05/20673, WO 03/14357, WO 03/13225, WO 03/143 56, WO 04/16073); enol c-oxalic acid-3-phosphate synthase (Epsps) inhibitor For example, glyphosate (see, for example, WO 92/00377); glutamine-synthase (GS) inhibitors, such as glufosinate (see, for example, European Patent EP-A- 0242236, EP-A-242246) or oxynil herbicide. The tolerance of several cultivated plants to herbicides has been conferred by conventional breeding (mutagenization) methods such as Clearfield® Brassica (Can〇la) to imidalin (eg, imazamox) Tolerance. Genetic engineering methods have been used to confer tolerance to herbicides (eg, soybean, cotton, corn, sugar beet, and canola) to herbicides (eg, glyphosate and glufosinate), some of which are commercially available under the trade name RoundupReady® ( Glyphosate) and LibertyLink® (glyphosate) are commercially available. The term "cultivated plants" as used herein additionally includes plants which are capable of synthesizing the following products by using recombinant DN a technology: one or more insecticidal proteins, in particular from the bacterium Bacillus, specifically from Bacillus thuringiensis Of (bacillus thuringiensis), such as a-endotoxin, such as CrylA (b), CrylA (c), CrylF, CryIF (a2), CryllA (b),

CrylllA、CrylllB(bl)或 Cry9c ;植物性殺昆蟲蛋白(VIp), 例如VIP1、VIP2、VIP3或VIP3A ;細菌聚居線蟲類之殺昆 蟲蛋白’例如發光桿菌屬(Photorhabdus)或致病桿菌屬 (Xenorhabdus);動物產生之毒素,例如礙子毒素、你蛛毒 素、黃蜂毒素、或其他昆蟲特異性神經毒素;真菌產生之 毒素’例如鏈黴菌(Streptomycete)毒素、植物凝集素,例 133661.doc •23- 200917962 如豌旦或大麥凝集素;凝集素;$白酶抑制劑,例如胰蛋 白酶抑制劑、絲胺酸蛋白酶抑制劑、帕它丁素(_‘)、 半耽胺酸蛋白酶抑制劑或木瓜蛋白酶抑制劑;核糖體失活 蛋白(RIP),例如萬麻毒素、玉米_RIp、相思豆毒素、絲瓜 素、皂草素或異株瀉根毒蛋白(bry〇din);類固醇代謝酶, 例如3-羥基類固醇氧化酶、脫皮素_1〇1&gt;_糖基_轉移酶、膽 固醇氧化酶、蜆化激素抑制劑或Hmg-CoA-還原酶;離子 通道阻滯劑’例如鋼或巧離子通絲滯劑;保幼激素能 酶,利尿激素受體(heiic〇kinin受體);二苯乙烯合酶、聯 苄基合酶、殼多糖酶或葡聚糖酶。在本發明上下文中,該 等殺昆蟲蛋白或毒素亦應明確理解為前毒素、雜化蛋白、 截短蛋白或經其他改良之蛋白。雜化蛋白之特徵係蛋白質 結構域之新組合(參見(例如)w〇 〇2/〇157〇1)。該等毒素或 能合成該等毒素之遺傳修飾植物之其他實例揭示於(例如)CrylllA, CrylllB (bl) or Cry9c; plant insecticidal protein (VIp), such as VIP1, VIP2, VIP3 or VIP3A; insecticidal proteins of bacterial nematodes such as Photorhabdus or Xenorhabdus ); toxins produced by animals, such as scorpion toxins, your spider toxins, wasp toxins, or other insect-specific neurotoxins; toxins produced by fungi such as Streptomycete toxins, plant lectins, 133661.doc •23 - 200917962 such as phloem or barley lectin; lectin; $ white enzyme inhibitor, such as trypsin inhibitor, serine protease inhibitor, statin (_'), semi-proline protease inhibitor or papaya Protease inhibitor; ribosome inactivating protein (RIP), such as urinary toxin, corn _RIp, abrin, loofah, saporin or lycopene (bry〇din); steroid metabolism enzymes, for example 3-hydroxysteroid oxidase, ecdysone_1〇1&gt;_glycosyl-transferase, cholesterol oxidase, sputum hormone inhibitor or Hmg-CoA-reductase; ion channel blocker' such as steel or clever Agents harness lag; juvenile hormone can be an enzyme, diuretic hormone receptors (heiic〇kinin receptor); stilbene synthase, bibenzylyl synthase, chitinases or glucanases. In the context of the present invention, such insecticidal proteins or toxins are also to be expressly understood to be protoxins, hybrid proteins, truncated proteins or other modified proteins. Hybrid proteins are characterized by a new combination of protein domains (see, for example, w〇 〇2/〇157〇1). Other examples of such toxins or genetically modified plants capable of synthesizing such toxins are disclosed, for example, in

歐洲專利第 EP-A 374 753 號、WO 93/007278、WOEuropean Patent No. EP-A 374 753, WO 93/007278, WO

95/34656、歐洲專利第EP_A 427 529號、歐洲專利第Ep_A 45 1 878 號、WO 03/01 881 0 及 WO 03/052073 中。產生該等 經遺傳修飾之植物之方法—般為熟習此項技術者已知且闡 述於(例如)上述公開案中。經遺傳修飾之植物中所含該等 木又**蛋白可針對來自某些節肢昆蟲分類群之害蟲保護產 生該等蛋白之植物,尤其針對曱蟲(鞘翅目、 蠅類(雙翅目(Diptera))、及蝴蝶及蛾(鱗翅目 (Lepidoptera)) ’且針對植物寄生性線蟲(線蟲綱 (Nematoda))。 13366 丨.doc -24- 200917962 另外包括利用重 組DNA技術能95/34656, European Patent No. EP_A 427 529, European Patent No. Ep_A 45 1 878, WO 03/01 881 0 and WO 03/052073. Methods of producing such genetically modified plants are generally known to those skilled in the art and are described, for example, in the above publication. The plants contained in genetically modified plants can protect plants that produce such proteins against pests from certain arthropod insect taxa, especially against aphids (coleoptera, flies (Diptera) )), and butterflies and moths (Lepidoptera) and target plant parasitic nematodes (Nematoda). 13366 丨.doc -24- 200917962 Also includes the use of recombinant DNA technology

本文所用術語”栽培植物 合成一或多稽卷白LV &amp; i 几至病疫黴菌(Phytophthora infestans)之源自墨西哥野生 馬鈴薯(Solanum buib〇castanum)之抗性基因)或溶菌酶 (例如能合成該等對諸如梨火疫病菌(Erwinia amyi_ra)等 細菌具有增強抗性之蛋白的馬鈐薯栽培變種)。產生該等 ”二这傳修飾植物之方法一般為熟習此項技術者所瞭解且闡 述於(例如)上文所提及之出版物中。 本文所用術語,,栽培植物,,另外包括如下之植物:其藉由 矛J用重組DNA技術能合成一或多種蛋白以增加彼等植物之 生產力(例如生物量生產、穀物產量、殿粉含量、油含量 或蛋白質含量)、對乾旱、鹽度或其他生長限制性環境因 素之耐受力、或對害蟲及真菌、細菌或病毒病原體之耐受 力。 本文所用術語”栽培植物”另外包括如下之植物:其藉由 利用重組DNA技術含有經改變量之内含物質或新内含物質 以特定地改良人類或動物營養,例如可產生促進健康之長 鏈ω-3脂肪酸或不飽和ω-9脂肪酸之油料作物(例如Nexera® 油菜)。 本文所用術語&quot;栽培植物&quot;另外包括如下之植物:其藉由 利用重組DNA技術含有經改變量之内含物質或新内含物質 133661 .doc -25- 200917962 以特定地改良原材料生產,例如可產生增加量支鏈殿粉之 馬鈴薯(例如Amflora®馬鈴薯)。 述’是里疋義中所提及之有機部分_與術語鹵素相-係 早獨列出之各群成員之統稱。前綴匕/^在每一情況下皆 指示基團中可能之碳原子數。 術語齒素在每一情況下皆表示氟 '溴、氣或碘,尤其 乱、氣或漠。 本文及烷氧基烷基、烷基胺基、二烷基胺基、烷基羰 基、烷硫基、烷基亞磺醯基及烷基磺醯基中之烷基部分中 所用術I吾”烷基”在每種情況下皆表示直鏈或具支鏈烷基, 其通*具有1至1 〇個碳原子,經常具有1至6個碳原子,較 佳具有1至4個碳原子。烷基之實例係甲基、乙基、正丙 基、異丙基、正丁基、2_ 丁基、異丁基、第三丁基、正戊 基、1-甲基丁基、2-甲基丁基、3 -曱基丁基、2,2-二曱基 丙基、1-乙基丙基、正己基、丨,^二甲基丙基、丨,2_二甲基 丙基曱基戊基、2 -曱基戊基、3 -甲基戊基、4 -甲基戊 基、I1·二甲基丁基、1,2-二甲基丁基、1,3-二曱基丁基、 2,2-二曱基丁基、2,3-二甲基丁基、3,3-二曱基丁基、1_乙 基丁基、2-乙基丁基、1,丨,2-三甲基丙基、丨,2,2_三甲基丙 基、1-乙基-1_曱基丙基、1_乙基_2_甲基丙基、正庚基、^ 甲基己基、2-甲基己基、3_甲基己基、4_曱基己基、5_甲 基己基、1-乙基戊基、2-乙基戊基、3 -乙基戍基、丨_丙基 戊基、正辛基、丨_曱基辛基、2_曱基庚基、丨_乙基己基、 2-乙基己基、12-二甲基己基、丙基戊基及2丙基戊 133661.doc -26- 200917962 基。 本文及鹵代烷硫基及函代烷基磺醯基之_代烷基部分中 所用術語&quot;鹵代烷基&quot;在每種情況下皆表示直鏈或具支鏈烷 基,其通常具有1至10個碳原子,經常具有丨至6個碳原 子,且其中此基團之氫原子部分或完全經齒素原子替代。 鹵代烷基部分較佳係選自C]_C4__代烷基,更佳係選自 C2鹵代炫基尤其係選自C i -C:2-氟代烧基,例如氟甲基、 二氟甲基 '三氟甲基、1-氟乙基、2-氟乙基、2,2-二氟乙 基、2,2,2-三氟乙基、五氟乙基、七氟異丙基及諸如此 類。 本文所用術語&quot;烷氧基&quot;在每種情況下皆表示直鏈或具支 鏈烷基,其經由氧原子鍵結且通常具有丨至丨〇個碳原子, 經常具有1至6個碳原子,較佳具有丨至4個碳原子。烷氧基 之實例係甲氧基、乙氧基、正丙氧基、異丙氧基、正丁氧 基、2-丁氧基、異丁氧基、第三丁氧基、戊氧基、&quot;基 丁氧基、2-甲基丁氧基、3_甲基丁氧基、2,2-二甲基丙氧 基、卜乙基丙氧基、己氧基、u二甲基丙氧基、以二甲 基丙氧基、1-甲基戊氧基、2_甲基戊氧纟、3_甲基戊氧 基、4-甲基戊氧基、u•二甲基丁氧基、二甲基丁氧 基I,3 一甲基丁氧基、2,2-二甲基丁氧基、2,3_二甲基丁 氧基、3,3-二甲基丁氧基乙基丁氧基、2_乙基丁氧 基、U,2-三甲基丙氧基、Hi三甲基丙氧基、卜乙基+ 甲基丙氧基、1-乙基_2-甲基丙氧基正庚氧基、卜甲基己氧 基、2-甲基己氧基、3_甲基己氧基、乒甲基己氧基、5·子 133661.doc -27- 200917962 基己氧基、1-乙基戊氧基、2-乙基戊氧基、3_乙基戊氧 基' 1-丙基戊氧基、正辛氧基、1-曱基辛氧基、2_甲基庚 氧基I -乙基己氣基、2-乙基己氧基、ι,2-二甲基己氧 基、1-丙基戊氧基及2-丙基戊氧基。 本文所用術語&quot;函代烷氧基&quot;在每種情況下皆表示直鏈或 具支鏈烷氧基,其具有丨至10個碳原子’經常具有丨至6個 碳原子,較佳具有丨至4個碳原子,且其中此基團之氫原子 部分或完全經函素原子替代,尤其經氣原子替代。齒代院 氧基部分較佳包括Cl々函代院氧基,尤其Ci_C2_氣代院 氧基,例如氟甲氧基、二氣甲氧基、三氣甲氧基、!_氣乙 氧基、2·氟乙氧基、2,2•二氟乙氧基、如.三氟乙氧基、 氟乙氧基、2备2,2_二說_乙氧基、2,2·二氣^•氣 乙乳基、2,2,2-三氣乙氧基、五氟乙氧基及諸如此類。 3 C!0環烷基_甲基之環烷基部分中所用術語”環 烧基&quot;在每種情況下皆表示單_或二環環脂族基團,其通常 W個C原子或3至6個。原子,例如環丙基、環丁 基、環戊基、環己基、環庚 衣厌基、%辛基、二環[2.1.1]己 二。一 庚基、二環[2.2·Π庚基、及二環[2.2.2]辛 用二及“代環燒基-甲基之南代環貌基部分中所 用術6口 _代環烷基,,在每種 基團,呈通當且古, 月况下白表示單-或二環環脂族 個广具有3至1〇個。原子或3至6個C原子,旦中至 少一個(例如!、2、3、〇 r 丁 /、Τ 主 _替代。實例係…A:由㈣替代’尤其由 亂% 丙基、1,2-、2,2-及 2,3-二 13366I.doc •28- 200917962 氣王衣丙基、122二备τ班τιο $ ,,二氟%丙基、2,2,3,3-四氟環丙基、1-及 -:¾丙基、丨,2_、2,2_及2,3_二氣環丙基”,2,三氯環 22土、、223,2,3,3~四氯環丙基、1-,2-及3-敦環戊基、1,2_、 2j2 2’3_ ' 3’3_、3,4·、2,5·二 I 環戊基、1~,2_及 3-氣環戊 基、1,2-、2,2-、2 3u , ,3,3_、3,4-、2,5-二氯環戊基及諸如 此類。 本文所用術語'’稀基”在每種情況下皆表示通常具有2至 10(例如2、3、4、5 a ^ ,, 、6、7或8)個C原子之單不飽和烴基, 例如乙稀基、稀丙基(2_丙稀小基)、卜丙稀小基、2_丙稀_ 2- 基、甲代烯丙基(2_甲基丙丄烯+基)、孓丁稀小基、3· 丁細-卜基、2-戊烯+基、3_戍稀·卜基、4_戊婦-卜基、卜 甲基丁 -2-烯-1·基、2_r其系1 &amp; 2乙基丙_2_烯_ι_基及諸如此類。 本文所用術語”炒·其&quot;大β 、基在母種情況下皆表示通常具有2至 1 0 (例如 2、3、4、5、ft、7 斗·。, 或8)個C原子之單不飽和烴基, 例如乙炔基、炔丙基(2_丙炔 炔1-基)、1-丙炔-1-基、1-曱基 丙-2-炔-1-基)、2-丁炔_丨_基、3_ 土 )』炔-1-基、I·戊炔-i基、 3- 戊炔-1 -基、4-戊炔-1 _基、i _甲其 丞i T基丁-2-炔-1-基、1_乙基 丙-2 -快-1-基及諸如此類。 本文所用術語&quot;(:丨-匕-烷盞其r p 4沉乳基-Cl~c4-烧基,,係指c〗_c4_烷 基’其中1個碳原子具有上破r ^β 噶上遮烷氧基。實例係ch2- och3、ch2-oc2h5、正丙氧基甲基、cH2 〇cH(cH3)2、正 丁氧基甲基、(1-甲基丙氧基)甲基、(2_甲基丙氧基)甲基、 CH2-〇C(CH3)3、2-(甲氧基)乙基、2_(乙氧基)乙基、2 (正 丙氧基)乙基、2·(1•甲基乙氧基)乙基、2_(正丁氧基)乙 I33661.doc -29- 200917962 基、2-(1-甲基丙氧基)乙基、2_(2_甲基丙氧基)乙基、2 (1,1-二甲基乙氧基)乙基、2_(甲氧基)丙基、2_(乙氧基)丙 基、2-(正丙氧基)丙基、2_(1_甲基乙氧基)丙基、2_(正丁 氧基)丙基、2-(1-甲基丙氧基)丙基、2_(2_甲基丙氧基)丙 基、2-(1,1 -二甲基乙氧基)丙基、3_(甲氧基)丙基、3_(乙氧 基)丙基、3-(正丙氧基)丙基、3_(1_曱基乙氧基)丙基、% r \ (正丁氧基)丙基、3-(1-曱基丙氧基)丙基、3 _(2_甲基丙氧 基)丙基、3·(1,^甲基乙氧基)丙基、2_(甲氧基)丁基、2_ (乙氧基)丁基、2-(正丙氧基)丁基、2_(1_曱基乙氧基)丁 基、2-(正丁氧基)丁基、2_(1_甲基丙氧基)丁基、2·(2_^'甲基 丙氧基)丁基、2-(1,1-二曱基乙氧基)丁基、3·(甲氧基)丁 基、3-(乙氧基)丁基、3-(正丙氧基)丁基、3_(1_曱基乙氧 基)丁基、3-(正丁氧基)丁基、3_(1•甲基丙氧基)丁基、% (2-曱基丙氧基)丁基、3-(Μ_二曱基乙氧基)丁基、4_(甲氧 基)丁基、4-(乙氧基)丁基、4-(正丙氧基)丁基、卜甲基 乙氧基)丁基、4-(正丁氧基)丁基、 基、4-(2-曱基丙氧基)丁基、4-(1,1_ 諸如此類。 4-(卜甲基丙氧基)丁 二曱基乙氧基)丁基及 本文所用術語&quot;烷硫基&quot;(烷基硫基:烷基_s_)係指直鏈或 具支鏈飽和烷基,其具有1至1〇個碳原子,較佳具有丄至^ 個碳原子(=C〗-C4-烷硫基)(如上所述),其係經由硫原子鍵 結。 本文所用術語”鹵代烷硫基,,係指上述烷硫基,其中氫原 子部分或元全經氣、氣、漠及/或換取代。 ” 133661.doc -30- 200917962 本文所用術語”烷基亞磺醯基&quot;(烷基次硫醯基:Ci_C6_烷 基-S( 0)-)係指直鏈或具支鏈飽和烧基(如上所述),其具 有1至10個碳原子,較佳具有1至4個碳原子(=C|-C4_烷基亞 %醯基),且在烷基中任一位置經亞磺醯基之硫原子鍵 結。 本文所用術語”鹵代烷基亞磺醯基&quot;係指上述烷基亞磺醯 基,其中氫原子部分或完全經氟、氣、溴及/或碘取代。 本文所用術語”烷基磺醯基,,(烷基·s(=0)2_)係指直鏈或具 支鏈飽和烷基,其具有丨至10個碳原子,較佳具有丨至4個 碳原子hq-C4-烷基磺醯基)(如上所述),其係在烷基中任 一位置經磺醯基之硫原子鍵結。 本文所用術語&quot;鹵代烷基磺醯基&quot;係指上述烷基磺醯基, 其中氫原子部分或完全經氟、氯、漠及/或埃取代。 V. 術語”雜環基”一般包括5_、6_、7_或8員單雜環基團及8 至10員二環雜環基團,單_及:環基團可為飽和、不飽和 或芳香族(=雜芳基)。單·及二環雜環基團通常包含】、2、3 或4個選自N、〇及8之雜原子作為環成員。 術語&quot;雜芳基”包括單環5—或6員雜芳香族基團,其包含 1: ':3或4個選自N、〇及8的雜原子作為環成員。… 貝雜方香族基團之實例包括吡啶基(即2_、%、或4-吡啶 ^、广定基(即2-、4_或5,基卜比嗪基、噠钱(即3-秦基^隹吩基(即2_或塞吩基)十南基(即或3-吱喃基)、料基(即2_或3+各基)…惡嗤基(即2_、3_或5 嗯。坐旬、異㈣基(即3—_或5_異^基)、㈣基(即2· 133661 .doc 200917962 、3-或5_㈣基)、異嗟唾基(即3…4_或5_異。塞唾基)”比 唑基(即1-、3-、4-或5-吼。坐基)、咪唾基(即卜2_、心或5 咪嗤基)、喔二嗤基(例如孓或^^⑷噪二峻基^或/ 〇,2,3_°惡二°坐)基、3_ 或 5_(1,2,4-°惡二唾)基、2-或 5-(1,3,4· 噻二。坐)基)、。塞二嗤基(例如2_或5_(1,3,4_嘆二唆)基、 5-(1,2,3-嗟二峻)基、3_或5_(1,2,4_噻二唾)基)、三嗤例 ㈣…抓或购^三^基^三^基叫^ 況…或则从三峻幻及四哇基⑼此或抓四唾 術語”雜芳基”亦包括8至1〇員二環雜芳香族基團q包 31、2或3個選自Ν'〇Β之雜原子作為環成員,/中5 或6貝雜芳香族環與苯環或與5•或6員雜芳香族基_人。 :本:或與5-或6員雜芳香族基團稍合之5_綱 並“ 本开夫南基、本开嘆吩基…引嗓基1唑 二开!哇基、笨并怖坐基、苯并嗯二。坐基、笨㈣ :土、本并喔嗪基、啥琳基、異啥啦基…票吟基、w 奈咬基、蝶咬基、口比咬并[3,2_d]喷口定基或口比咬并味’ 諸如此類。兮笙抽人 土及 …合雜芳基可經由5-或6員雜芳香族環之 部八衣’、子或經由稠合苯基部分之碳原子鍵結至分子其餘 s飽和或不飽和雜環之實例包含飽和或不飽和非芳香族雜 環’例如π比略哈其 w 、雜 疋基、π比唑淋基、咪唑琳基、0比 氫呋喃基、-H。土 土、四 基、硫味基二喃基、U3_二氧戊環基、間二氣環戍稀 —氧°塞吩基、鳴也咬基、異嗯唾D定基、過 啉基、異噁唑嗾I ^ °坐 琳基、°塞。坐淋基、異嗟嗅琳基、。塞唾σ定芙 133661.doc -32- 200917962 異噻唑啶基、伸氧硫味基、六氫吡啶基、六氫吡嗪基、吡 喃基、二氫吡喃基、四氫吡喃基、及丨,4-二噁烷基、 噻喃基、二氫噻喃基、四氫噻喃基、嗎啉基、噻嗪基及諸 如此類。亦包含1或2個羰基作為環成員之雜環之實例包含 吡咯啶-2-嗣基、吡咯啶_2,5_二酮基、味唑啶_2_酮基、嚼 唑啶-2-酮基、嚙唑啶-2-_基及諸如此類。 術語”苯基-cvc4道基”及&quot;苯氧基_Ci_C4_烧基”分別指苯 基或苯氧基,其係經由Cl_C4_烷基(尤其曱基(=雜芳基甲 基))鍵結至分子之其餘部分,實例包括节基、丨苯乙基、 2-苯乙基、2-苯氧基乙基等。 術語”雜環-CVCV烧基&quot;及,,雜芳基_Ci_C4_烧基&quot;分別指如 上文所疋義之雜%基或雜芳基,其經由Ci_Cc烷基(尤其甲 基(分別=雜環基甲基或雜芳基甲基))鍵結至分子之其餘部 分。 徵 卜又關於式I或II化合物 ▼人玉,个贫。月用迷汉乃法之特As used herein, the term "cultivating plants synthesize one or more LV & i to Phytophthora infestans derived from the wild potato (Solanum buib〇castanum) resistance gene) or lysozyme (for example, can synthesize A cultivar of horse mash that has an enhanced resistance to a bacterium such as Erwinia amyi_ra. The method of producing such a modified plant is generally known to those skilled in the art and is described in (for example) in the publication mentioned above. The term, cultivated plant, as used herein, additionally includes a plant which, by means of recombinant DNA technology, can synthesize one or more proteins to increase the productivity of such plants (eg biomass production, grain yield, meal content, Oil content or protein content), tolerance to drought, salinity or other growth limiting environmental factors, or tolerance to pests and fungal, bacterial or viral pathogens. The term "cultivating plants" as used herein additionally includes plants which, by using recombinant DNA techniques, contain altered amounts of inclusions or new inclusions to specifically modify human or animal nutrition, for example, to produce long chains that promote health. Oil crops of omega-3 fatty acids or unsaturated omega-9 fatty acids (eg Nexera® canola). The term &quot;cultivating plants&quot; as used herein, additionally includes plants which, by using recombinant DNA techniques, contain altered amounts of contained or new contents 133661.doc -25-200917962 to specifically improve the production of raw materials, for example A potato (eg, Amflora® potato) that produces an increased amount of branched powder. The statement 'is the organic part mentioned in Li Yiyi _ and the term halogen phase-- is the collective name of each group member listed earlier. The prefix 匕/^ indicates in each case the number of possible carbon atoms in the group. The term dentate in each case means fluorine 'bromo, gas or iodine, especially chaotic, gas or desert. And the alkyl moiety used in the alkoxyalkyl, alkylamino, dialkylamino, alkylcarbonyl, alkylthio, alkylsulfinyl and alkylsulfonyl groups" The alkyl group means, in each case, a straight-chain or branched alkyl group having from 1 to 1 carbon atoms, often having from 1 to 6 carbon atoms, preferably from 1 to 4 carbon atoms. Examples of alkyl groups are methyl, ethyl, n-propyl, isopropyl, n-butyl, 2-butyl, isobutyl, tert-butyl, n-pentyl, 1-methylbutyl, 2-methyl Butyl, 3-nonylbutyl, 2,2-dimercaptopropyl, 1-ethylpropyl, n-hexyl, hydrazine, dimethyl propyl, hydrazine, 2 dimethyl propyl hydrazine Pentyl, 2-mercaptopentyl, 3-methylpentyl, 4-methylpentyl, I1. dimethylbutyl, 1,2-dimethylbutyl, 1,3-didecyl Butyl, 2,2-dimercaptobutyl, 2,3-dimethylbutyl, 3,3-didecylbutyl, 1-ethylbutyl, 2-ethylbutyl, 1, hydrazine , 2-trimethylpropyl, hydrazine, 2,2-trimethylpropyl, 1-ethyl-1-mercaptopropyl, 1-ethyl-2-methylpropyl, n-heptyl, ^ Methylhexyl, 2-methylhexyl, 3-methylhexyl, 4-mercaptohexyl, 5-methylhexyl, 1-ethylpentyl, 2-ethylpentyl, 3-ethylindenyl, hydrazine _propylpentyl, n-octyl, 丨-mercaptooctyl, 2-fluorenylheptyl, 丨_ethylhexyl, 2-ethylhexyl, 12-dimethylhexyl, propylpentyl and 2 Kee 133661.doc -26- 200917962 base. The term &quot;haloalkyl&quot; as used herein and in the alkylene moiety of haloalkylthio and haloalkylsulfonyl, in each case denotes a straight or branched alkyl group, which typically has from 1 to 10 One carbon atom, often having from 丨 to 6 carbon atoms, and wherein the hydrogen atom of this group is partially or completely replaced by a dentate atom. The haloalkyl moiety is preferably selected from the group consisting of C]-C4__alkyl, more preferably from C2 halo, especially from C i -C: 2-fluoroalkyl, such as fluoromethyl, difluoromethyl 'Trifluoromethyl, 1-fluoroethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, pentafluoroethyl, heptafluoroisopropyl and And so on. The term &quot;alkoxy&quot; as used herein, in each case, denotes a straight or branched alkyl group which is bonded via an oxygen atom and which typically has from one to one carbon atom, often from 1 to 6 carbons. The atom preferably has from 丨 to 4 carbon atoms. Examples of alkoxy groups are methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, 2-butoxy, isobutoxy, tert-butoxy, pentyloxy, &quot;Gytyloxy, 2-methylbutoxy, 3-methylbutoxy, 2,2-dimethylpropoxy, bethylpropoxy, hexyloxy, u-dimethylpropoxy With dimethylpropoxy, 1-methylpentyloxy, 2-methylpentyloxy, 3-methylpentyloxy, 4-methylpentyloxy, u•dimethylbutoxy, Dimethylbutoxy 1,3 methylbutoxy, 2,2-dimethylbutoxy, 2,3-dimethylbutoxy, 3,3-dimethylbutoxyethyl Butoxy, 2-ethylbutoxy, U,2-trimethylpropoxy, Hi trimethylpropoxy, bethyl + methylpropoxy, 1-ethyl 2 -methylpropoxy Base n-heptyloxy, benzyl hexyloxy, 2-methylhexyloxy, 3-methylhexyloxy, phenethyl hexyloxy, 5· 133661.doc -27- 200917962 hexyloxy, 1 -ethylpentyloxy, 2-ethylpentyloxy, 3-ethylpentyloxy' 1-propylpentyloxy, n-octyloxy, 1-decyloctyloxy, 2-methylheptyloxy I-ethylhexyl, 2-ethylhexyl Group, iota, 2- dimethyl-hexyloxy group, 1-propyl and 2-propyl-pentyloxy group, pentyloxy group. The term &quot;the alkoxy group&quot; as used herein, in each case, denotes a straight-chain or branched alkoxy group having from 10 to 10 carbon atoms, often having from 丨 to 6 carbon atoms, preferably having丨 to 4 carbon atoms, and wherein the hydrogen atom of this group is partially or completely replaced by a hydroxyl atom, especially by a gas atom. Preferably, the oxy moiety of the dentate includes a Cl 々 代 代 ethoxy group, especially a Ci_C2 _ gas, such as fluoromethoxy, dimethoxy, trimethoxy, _ gas ethoxy, 2 · fluoroethoxy, 2, 2 • difluoroethoxy, such as .trifluoroethoxy, fluoroethoxy, 2, 2, 2 _ _ ethoxy, 2 , 2· 2 gas ^ • gas ethyl lactyl, 2, 2, 2-trisethoxy, pentafluoroethoxy and the like. The term "cycloalkyl" used in the 3 C!0 cycloalkyl-methyl cycloalkyl moiety means, in each case, a mono- or bicyclic cycloaliphatic group, usually W C atoms or 3 Up to 6. Atoms such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptin, % octyl, bicyclo [2.1.1] hexamethylene, monoheptyl, bicyclo [2.2 · Πheptyl, and bicyclo [2.2.2] octyl 2 and "cyclohexyl-methyl" in the southern ring of the ring-based part of the 6-hydroxy-alkyl group, in each group, It is generally and ancient, and the white under the moon indicates that the mono- or bicyclic ring aliphatics have a total of 3 to 1 。. An atom or 3 to 6 C atoms, at least one of the deniers (eg, !, 2, 3, 〇r ding /, Τ main _ substitution. Examples are... A: replaced by (d) 'especially by chaotic % propyl, 1, 2 -, 2,2- and 2,3-two 13366I.doc •28- 200917962 gas king propyl, 122 two preparation τ class τιο $ ,, difluoro% propyl, 2,2,3,3-tetrafluoro Cyclopropyl, 1- and -: 3⁄4 propyl, hydrazine, 2_, 2, 2_ and 2,3_di-cyclopropyl propyl", 2, trichlorocyclocarbonate 22, 223, 2, 3, 3~ Tetrachlorocyclopropyl, 1-, 2- and 3-Dencyclopentyl, 1,2_, 2j2 2'3_ '3'3_, 3,4·, 2,5·II Icyclopentyl, 1~, 2_ and 3-cyclopentyl, 1,2-, 2,2-, 2 3u , , 3,3_, 3,4-, 2,5-dichlorocyclopentyl and the like. The term '' is used herein. "Thinyl" means, in each case, a monounsaturated hydrocarbon group typically having 2 to 10 (eg 2, 3, 4, 5 a ^ , , 6, 7, or 8) C atoms, such as ethylene, dilute Propyl (2-propylene small base), propylene small base, 2-propylene -2-yl, methallyl (2-methylpropenene + base), butyl butyl group, 3 · Dingzhi-Buji, 2-pentene+yl, 3_戍稀·卜基, 4_戊妇-卜基, 卜 methylbut-2- -1·基, 2_r, 1 & 2 ethylpropan-2-ene_ι_yl, and the like. The term "fried" is used herein to mean "large beta", and in the case of the parent species, it usually has 2 to 1 0 (eg 2, 3, 4, 5, ft, 7 hoppers, or 8) monounsaturated hydrocarbon groups of C atoms, such as ethynyl, propargyl (2-propyne-1-yl), 1 -propyn-1-yl, 1-mercaptopropan-2-yn-1-yl), 2-butyne-indenyl, 3_a),yn-1-yl, I.pentyne-i, 3-pentyne-1 -yl, 4-pentyne-1 yl, i _methyl 丞 i T T-but-2-yn-1-yl, 1-ethylpropan-2-cyclo-1-yl and And the like. The term &quot;(:丨-匕-alkane rp 4 milyl-Cl~c4-alkyl, referred to as c _c4_alkyl', wherein one carbon atom has an upper r ^β Indole alkoxy. Examples are ch2- och3, ch2-oc2h5, n-propoxymethyl, cH2 〇cH(cH3)2, n-butoxymethyl, (1-methylpropoxy)methyl , (2_methylpropoxy)methyl, CH2-〇C(CH3)3, 2-(methoxy)ethyl, 2-(ethoxy)ethyl, 2 (n-propoxy)ethyl , 2·(1•methylethoxy)ethyl, 2_(n-butoxy)ethyl I33661.doc -2 9- 200917962, 2-(1-methylpropoxy)ethyl, 2-(2-methylpropoxy)ethyl, 2 (1,1-dimethylethoxy)ethyl, 2_( Methoxy)propyl, 2-(ethoxy)propyl, 2-(n-propoxy)propyl, 2-(1-methylethoxy)propyl, 2-(n-butoxy)propyl, 2-(1-methylpropoxy)propyl, 2-(2-methylpropoxy)propyl, 2-(1,1-dimethylethoxy)propyl, 3-(methoxy) Propyl, 3-(ethoxy)propyl, 3-(n-propoxy)propyl, 3-(1-decylethoxy)propyl, % r \ (n-butoxy)propyl, 3- (1-mercaptopropoxy)propyl, 3-(2-methylpropoxy)propyl, 3·(1,^methylethoxy)propyl, 2-(methoxy)butyl, 2-(Ethoxy)butyl, 2-(n-propoxy)butyl, 2-(1-decylethoxy)butyl, 2-(n-butoxy)butyl, 2-(1-methyl) Propoxy)butyl, 2·(2_^'methylpropoxy)butyl, 2-(1,1-didecylethoxy)butyl, 3(methoxy)butyl, 3 -(ethoxy)butyl, 3-(n-propoxy)butyl, 3-(1-decylethoxy)butyl, 3-(n-butoxy)butyl, 3-(1•methyl C Oxy)butyl, % (2-mercaptopropoxy)butyl, 3-(anthracene-diylethoxy)butyl, 4-(methoxy)butyl, 4-(ethoxy) Butyl, 4-(n-propoxy)butyl, methylethyloxy)butyl, 4-(n-butoxy)butyl, benzyl, 4-(2-mercaptopropoxy)butyl, 4 -(1,1_ and so on. 4-(Bypropylpropoxy)butyldinylethoxy)butyl and the term &quot;alkylthio&quot; (alkylthio:alkyl_s_) as used herein means straight-chain or branched-chain saturated alkane A group having from 1 to 1 carbon atoms, preferably having from 丄 to ^ carbon atoms (=C -C4-alkylthio) (as described above), which is bonded via a sulfur atom. The term "haloalkylthio" as used herein, refers to an alkylthio group as defined above, wherein the hydrogen atom is partially or partially replaced by gas, gas, indifference and/or substitution. 133661.doc -30- 200917962 The term "alkyl" is used herein. Sulfhydryl&quot; (alkyl thiopurinyl: Ci_C6_alkyl-S(0)-) means a straight or branched saturated alkyl group (as described above) having from 1 to 10 carbon atoms, It preferably has from 1 to 4 carbon atoms (=C|-C4_alkyl hydrazone) and is bonded via a sulfur atom of a sulfinyl group at any position in the alkyl group. The term "haloalkyl" is used herein. Sulfoinyl&quot; refers to the above alkylsulfinyl group in which the hydrogen atom is partially or completely substituted with fluorine, gas, bromine and/or iodine. The term "alkylsulfonyl," (alkyl s(=0)2_), as used herein, refers to a straight or branched saturated alkyl group having from 10 to 10 carbon atoms, preferably from 4 to 4 carbon atoms. a carbon atom hq-C4-alkylsulfonyl) (as described above) which is bonded at any position in the alkyl group via a sulfur atom of a sulfonyl group. The term &quot;haloalkylsulfonyl&quot; Refers to the above alkylsulfonyl group, wherein the hydrogen atom is partially or completely substituted by fluorine, chlorine, indifference and/or angstrom. V. The term "heterocyclyl" generally includes a 5-, 6-, 7- or 8-membered monoheterocyclic group. And 8 to 10 membered bicyclic heterocyclic groups, mono- and: ring groups may be saturated, unsaturated or aromatic (=heteroaryl). Mono- and bicyclic heterocyclic groups usually contain], 2 3 or 4 heteroatoms selected from N, oxime and 8 as ring members. The term &quot;heteroaryl" includes a monocyclic 5- or 6-membered heteroaromatic group containing 1: ':3 or 4 Heteroatoms from N, 〇 and 8 serve as ring members. Examples of the beixiangfang group include pyridyl (ie, 2, %, or 4-pyridine^, broadly based (ie, 2-, 4 or 5, kibazine, 哒 (ie 3- Qin) a thiol group (ie, 2 or a sylylene group), a sulphonyl group (ie, 2 or 3+ groups). 5 um. Sit, different (four) base (ie 3 - _ or 5 _ ^ base), (4) base (ie 2 · 133661 .doc 200917962, 3- or 5_ (four) base), iso-salt base (ie 3...4_ Or 5_iso. Sesinyl)"Bizozolyl (ie 1-, 3-, 4- or 5-anthracene. Sodium), Sodium sulphate (ie Bu 2_, Heart or 5 mercapto), 喔二嗤 base (such as 孓 or ^^ (4) noise two Junji ^ or / 〇, 2, 3_ ° 恶二° sit) base, 3_ or 5_(1,2,4-° dioxin) base, 2- or 5 - (1,3,4·thiadi. sit) base), thiophene (for example, 2_ or 5_(1,3,4_ 唆 唆) base, 5-(1,2,3-嗟) (2) base, 3_ or 5_(1,2,4_thiadisyl), three examples (four)... grab or buy ^^^^^^^^^^^^^^^^^^ Siwaji (9) This or scratching the term "heteroaryl" also includes 8 to 1 member of the bicyclic heteroaromatic group q package 31, 2 or 3 A hetero atom selected from Ν'〇Β as a ring member, /5 or 6-shell heteroaromatic ring with a benzene ring or with a 5 or 6-membered heteroaromatic group.: Ben: or with 5 or 6 members The heteroaromatic group is slightly combined with the 5_ class and "this Kaifu Nanji, Ben Kai sing sing... 嗓 嗓 1 azole 2 open! Wow, stupid and terrible base, benzo y. Stupid (4): soil, this oxazinyl, 啥琳基, iso- 啥 基 ... 吟 ... ... ... ... ... 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 ' 诸如 人 人 及 及 及 及 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合 合Examples of the unsaturated heterocyclic ring include a saturated or unsaturated non-aromatic heterocyclic ring 'e.g., π, sirhas, w, fluorenyl, π, oxazolidine, imidazolinyl, 0, hydrogenfuranyl, -H. , tetrakisyl, sulphur-based di-amyl, U3_dioxolanyl, m-cyclohexane, di-oxygen, thiophene, thiophene, sulphate, porphyrin, isoxazole嗾I ^ ° sit on the base, ° plug. sit on the base, different scent Olivin塞 σ σ 定 133661.doc -32- 200917962 Isothiazolidinyl, thioxanthene, hexahydropyridyl, hexahydropyrazinyl, pyranyl, dihydropyranyl, tetrahydropyran And hydrazine, 4-dioxoalkyl, thiopyranyl, dihydrothiopyranyl, tetrahydrothiopyranyl, morpholinyl, thiazinyl and the like. Also contains 1 or 2 carbonyl groups as ring members. Examples of the ring include pyrrolidin-2-indenyl, pyrrolidine-2,5-dione, mezolidine-2-keto, cherazazole-2-one, oroxazolidine-2-yl and And so on. The terms "phenyl-cvc4) and "phenoxy-Ci_C4_alkyl" mean phenyl or phenoxy, respectively, via Cl_C4_alkyl (especially fluorenyl (=heteroarylmethyl)) Bonded to the rest of the molecule, examples include a benzyl group, anthranilyl, 2-phenethyl, 2-phenoxyethyl, etc. The term "heterocycle-CVCV alkyl" &quot;, heteroaryl_ Ci_C4_alkyl group&quot; respectively refers to a hetero- or heteroaryl group as defined above, which is bonded to the molecule via a Ci_Cc alkyl group (especially methyl (hetero = heterocyclylmethyl or heteroarylmethyl)) The rest. The levy is also about the compound of formula I or II. Moonlight

、及本發明組合物之較佳實施例所作之評述係單獨有效 的且-較佳地_在彼此組合時有效。 /發明較佳實施例係關於式Ιπ比唾化合物、其鹽、其队 乳化物及該等化合物之方法及應用。式〗化合物中,較佳 者係式I中之X1為氧、硫或部分N_Rla之彼等化合物。尤佳 者係其中χ1為氧之彼等式I化合物。 在其中X為NR之式!化合物中,具體實施例係關於彼 化合物,其中Ria^c /、u係q-cv烧基、C】_C6_鹵代烧基 環燒基、C3-C6-環烧美甲其 r ^ 6 6衣沉基曱基、CyCV鹵代環烷基、CyCp烯 J3366l.doc •33- 200917962 基c2 (:6-南代稀基、C2_C6_块基、Ci_C4_烧氧基_Ci_C6j 基苯基、雜芳基、苯基-C,-C4_烷基及雜芳基_Cl_C4-烷 基,其中上述最後4個基團之芳香族環可未經取代或可具 有1、2、3、4或5個彼此獨立地選自由以下組成之群之取 代基:函素、氰基、硝基、G-CV烷基、Cl_C4_齒代烷 基Cl-C4_烷氧基及G-C:4-鹵代烷氧基;或部分〇Ra。具體 而σ ,R係C〗-C6-烷基、c3-C6-環烷基曱基、C3_C6_烯 基C3_C6_炔基、C^CV烷氧基-CVC4-烷基或部分〇Ra,其 中R係如上文所定義且具體而言係選自Ci_C6_烷基、 CV%烷基甲基、C3_C0_烯基、C3_C6_炔基及Ci_C4_烷氧基_ C 1 -C4-烧基。 式I化合物中,較佳者係彼等化合物,其中Rl係氫、 CN CVCw-烧基、Cj-C^o-鹵代院基、c2-C10-稀基、C2_ Ci〇-鹵代烯基、c2-C10-炔基、C^-CV烷氧基-c^-Cw烷基、 c】-c4-伸烷基-CN、0Ra、C(Y)Rb、c(Y)〇Rc^s(〇)2Rd。更 佳者係式i化合物,其中R〗係氫、Ci_Ci〇_烷基、Ci_Ci〇_鹵 代烷基、C2-C10-烯基、c2_Cl0_鹵代烯基、c2_Ci〇_炔基、 q-C4-烧氧基-C^Cm-烷基或CVC4·伸烷基-CN,具體而言 係氫、(VC3-烷基或Cl_C4_伸烷基_CN,尤其氫、曱基或乙 基。 本發明另一實施例係關於式ii吡唑化合物、其鹽、其N_ 氧化物及該等化合物之方法及應用。在式〗〗化合物中,較 佳者係式II中之X2為0Rh或之彼等化合物。在該等化 合物中,R2a較佳為Cl_C6_烷基、C3-C6•烯基、C3_C6_块 133661.doc -34- 200917962 基、CVCV環烷基甲基或Cl_C4_烷氧基· 10 基。另 實施例係關於式I化合物,其中χ2传NR2bp2c L 2b ” K 。在該等實施 例中’ R及Re較佳係彼此獨立地選自 ^ 目 L】_C6-燒基、C3-C6· 環烧基甲基或Cl々烧氧基H㈣及R2e與其所鍵結 之乳原子一起形成鍵結氮之飽和5_或6員雜環,其可包含The comments made by the preferred embodiments of the compositions of the invention are individually effective and - preferably - effective when combined with one another. The preferred embodiment of the invention relates to a method and application of the formula Ιπ to a salivation compound, a salt thereof, a group emulsion thereof, and the like. Among the compounds of the formula, X1 in the formula I is preferably a compound of oxygen, sulfur or a part of N_Rla. Particularly preferred are those compounds of formula I wherein χ1 is oxygen. In which X is the NR type! Among the compounds, specific examples relate to the compound, wherein Ria^c /, u is a q-cv alkyl group, C]_C6_haloalkylcycloalkyl, C3-C6-ring-burning manicure, its r^6 6 garment Substrate, CyCV halocycloalkyl, CyCpene J3366l.doc •33- 200917962 base c2 (:6-Southern rare base, C2_C6_ block, Ci_C4_alkoxy_Ci_C6j phenyl, heteroaryl a phenyl group, a phenyl-C, a C4 alkyl group, and a heteroaryl group _Cl_C4-alkyl group, wherein the aromatic ring of the last four groups described above may be unsubstituted or may have 1, 2, 3, 4 or 5 Substituents independently selected from the group consisting of: a phytase, a cyano group, a nitro group, a G-CV alkyl group, a Cl_C4_dentate alkyl group, a C-C4 alkoxy group, and a GC: 4-haloalkoxy group; Or a partial 〇Ra. Specifically, σ, R is a C-C6-alkyl group, a c3-C6-cycloalkylindenyl group, a C3_C6-alkenyl C3_C6-alkynyl group, a C^CV alkoxy group-CVC4-alkyl group or Part 〇Ra, wherein R is as defined above and in particular is selected from Ci_C6_alkyl, CV% alkylmethyl, C3_C0-alkenyl, C3_C6-alkynyl and Ci_C4_alkoxy_C1-C4 a compound of the formula I, preferably a compound thereof, wherein R1 is hydrogen, CN CVCw-alkyl, C jC^o-halogenated, c2-C10-dilutyl, C2_Ci-haloalkenyl, c2-C10-alkynyl, C^-CV alkoxy-c^-Cw alkyl, c]- C4-alkylene-CN, 0Ra, C(Y)Rb, c(Y)〇Rc^s(〇)2Rd. More preferred are compounds of formula i, wherein R is hydrogen, Ci_Ci〇_alkyl, Ci_Ci 〇_haloalkyl, C2-C10-alkenyl, c2_Cl0_haloalkenyl, c2_Ci〇-alkynyl, q-C4-alkoxy-C^Cm-alkyl or CVC4·alkylene-CN, specifically Hydrogen, (VC3-alkyl or Cl_C4_alkylene-CN, especially hydrogen, decyl or ethyl. Another embodiment of the invention relates to a pyrazole compound of the formula ii, a salt thereof, an N-oxide thereof and And the method and application of the compound. In the formula, the preferred formula X2 is 0Rh or a compound thereof. Among the compounds, R2a is preferably Cl_C6_alkyl, C3-C6• Alkenyl, C3_C6_block 133661.doc -34- 200917962, CVCV cycloalkylmethyl or Cl_C4_alkoxy-10-yl. Further examples relate to compounds of formula I wherein χ2 carries NR2bp2c L 2b ” K. In these examples, 'R and Re are preferably selected independently of each other from the group L. _C6-alkyl, C3-C6. cycloalkylmethyl Or Cl 々 alkoxy H (tetra) and R 2e together with the milk atom to which they are bonded form a saturated nitrogen 5- or 6-membered heterocyclic ring of a bonded nitrogen, which may comprise

另一選自〇、S及N之雜原子,例如NR2bR2c S 你1 - π比》各α定基、 1 -六虱η比π定基、1 -六氫π比π秦基、心4被其+ / 馬啉基或4-硫嗎啉基。 在本發明方法及應用及化合物中 中之R2係選自氫、甲基、二氟曱基 一II甲氧基及三氟甲氧基之化合物 在本發明方法及應用及化合物中 中之R3係選自氫、甲基、二氟曱基 車父^圭者係其中式I及II 三氧甲基、甲氧基、 方法及應用。 較佳者係其中式I及II 二氟曱基、甲氧基、 f 一氟甲氧基及二氟甲氧基之化合物、方法及應用。 具體而言,式I及II之基團R2或R3中至少一個係氫。本發 明極佳實施例係關於式I及Π化合物及其鹽,其中尺2及R3二 者皆為氫。Another hetero atom selected from ruthenium, S and N, such as NR2bR2c S, 1 - π ratio, each α-based group, 1 - hexa-n-n ratio π-base, 1 - hexahydro-π ratio π-methyl group, heart 4 is + / Phyrinol or 4-thiomorpholinyl. R2 in the methods, uses and compounds of the invention are selected from the group consisting of hydrogen, methyl, difluoroindolyl-IImethoxy and trifluoromethoxy compounds in the methods and applications of the invention and in the compounds R3 It is selected from the group consisting of hydrogen, methyl, and difluoroindolyl. It is a trimethoxymethyl group, a methoxy group, a method, and an application thereof. Preferred are compounds, methods and uses of the formulas I and II of difluoroindolyl, methoxy, f-fluoromethoxy and difluoromethoxy. In particular, at least one of the groups R2 or R3 of the formulae I and II is hydrogen. An excellent embodiment of the invention relates to Formula I and indole compounds and salts thereof, wherein both Scale 2 and R3 are hydrogen.

本發明另一較佳實施例係關於式丨及π化合物及其鹽及其 Ν-氧化物,其中R2係氫且R3係選自氫、甲基、二氟甲基、 三氟曱基、曱氧基、二氟甲氧基及三氟曱氧基。本發明另 一較佳實施例係關於式!及Π化合物及其鹽,其中R3係氣且 R-係選自氫、甲基、二氟曱基、三氟甲基、甲氧基、二氟 甲氧基及三氟甲氧基。 本發明較佳實施例係關於式I及II吡唑化合物、其鹽、其 N-氧化物及該等化合物之方法及應用,其中a係基團Ai。 133661 .doc -35- 200917962 其:較佳者係式1化合物’其中X1、R丨、R2及R3係如上文 所定義且尤其具有一種較佳含義。 在其中A係基團A1之式1及11吡唑化合物中,R4]及R5丨較 =彼此獨立地選自氫、鹵素、CN、Cl-Cl〇_烷基、c3_Ci〇_ 環烷基、C2_Ciq_烯基及Ci_Ciq_炔基,其中上述最後4個基 團中之脂肪族或環狀部分可未經取代、可部分或完全鹵化 或可具有1或2個相同或不同取代基Ry。具體而言,R4,及 R51係彼此獨立地選自氫、_素、CN、Ci_c4_烷基、c丨_C4-白代烧基C3-C6_環烧基及C3_C6_鹵代環烧基,且更佳係 選自氫、鹵素、CN、CH3、CH2F、CHF2及 cf3。 較佳地,基團R4〗&amp;R51中至少一個或兩個為氫。具體而 言’ R41或R51係選自_素、CN、Ci_Ci〇_烧基、C3_Ci。·環烧 基、C2_c1(r烯基及C2_Ci〇_炔基,其中上述最後4個基團中 之脂肪族或環狀部分可未經取代、可部分或完全鹵化或可 具有1或2個相同或不同取代基Ry,同時基團或rS1中另 一個係氫或鹵素,尤其為氫。更佳地,R4 1或R5 !係選自鹵 素、CN、c〗-c4-烧基、c〗-c4-鹵代烧基、c3-c6-環烷基及 c3-c6-鹵代環烷基’且最佳係選自鹵素、CN、Ch3、 CH2F、CHF2及CF3 ’同時基團R41或R51中另—個係氫。 在其中A係基團A1之式I及I ]&gt;比。坐化合物中,r6 1較佳係 選自由以下組成之群:Cl_Cl〇_烷基、Cl-C〗〇_鹵代烷基、 C3-C10-環烧基、(1:3-(310-_代環烧基、c3-C10-環烧基曱基、 C3-Ci〇-鹵代環烧基曱基、C2-C10-烯基、c2-cl0_ _代烤基、 C1-C4 -炫•氧基-C^-Cw烧基、苯基、节基、笨氧基_曱基、 133661.doc -36- 200917962 5-或6貝雜芳基、5_或6員雜芳基甲基,其中上述最後5個基 團中之(雜)芳香族環可未經取代或可具有1、2、3、4或5個 相同或不同取代基RX,其係如上文所定義且較佳係選自函 素、c,-c4-烧基、C】_C4_函代烧基、Ci_C4_燒氧基、ci&lt;-鹵代貌6氧基、(VC4-烷基磺醯基及Cl_C4_鹵代烷基磺醯 基。更佳為c〗-C4·烷基或C]_C4_鹵代烷基,尤其為甲 基'乙基、正丙基、異丙基、二氟甲基、三氟甲基、2_氟 土 ,—氟乙基及2,2,2 -二乙基。同樣較佳者係其中 A係基團A1之式!及„化合物,其中及RSi係如本文所定 義且其中R係選自苯基、节基及5_或6員雜芳基,尤其吼 啶基、吡唑基、咪唑基、噁唑基、噻唑基 '異噁唑基、異 噻唑基、1,2,4-噻二唑基、l,3,4-噻二唑基、三唑 基、1,2,4-三唑基或四唑基,其中苯基、苄基及5_或6員雜 芳基中之芳香族部分未經取代或可具有1、2或3個相同或 不同取代基Rx,其係如上文所定義且較佳係選自鹵素、 G-CV炫基、CVCV鹵代烧基、CrCV烧氧基、 烧氧基、CVCV烷基續醯基、及C^-CU-鹵代烧基績醯基。 適宜基團A1之實例係以下式之基團:Al a、Al b、Another preferred embodiment of the present invention relates to a ruthenium compound and a ruthenium compound thereof, and a ruthenium-oxide thereof, wherein R2 is hydrogen and R3 is selected from the group consisting of hydrogen, methyl, difluoromethyl, trifluoromethyl, fluorene Oxy, difluoromethoxy and trifluoromethoxy. Another preferred embodiment of the invention is related to the formula! And a hydrazine compound and a salt thereof, wherein R3 is a gas and the R-line is selected from the group consisting of hydrogen, methyl, difluorodecyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy. Preferred embodiments of the invention are directed to a pyrazole compound of formula I and II, a salt thereof, an N-oxide thereof, and methods and uses thereof, wherein a is a group Ai. 133661 .doc -35- 200917962 It is preferred that the compound of formula 1 is wherein X1, R丨, R2 and R3 are as defined above and in particular have a preferred meaning. In the pyrazole compounds of the formula 1 and 11 in the A group A1, R4] and R5 are more independently selected from the group consisting of hydrogen, halogen, CN, Cl-Cl〇-alkyl, c3_Ci〇_cycloalkyl, C2_Ciq_alkenyl and Ci_Ciq_alkynyl, wherein the aliphatic or cyclic moiety of the last four groups described above may be unsubstituted, partially or fully halogenated or may have 1 or 2 identical or different substituents Ry. Specifically, R4 and R51 are independently selected from the group consisting of hydrogen, _, CN, Ci_c4_alkyl, c丨_C4-white alkyl C3-C6_cycloalkyl and C3_C6_halocycloalkyl More preferably, it is selected from the group consisting of hydrogen, halogen, CN, CH3, CH2F, CHF2, and cf3. Preferably, at least one or both of the groups R4 &amp; R51 are hydrogen. Specifically, 'R41 or R51 is selected from the group consisting of _, CN, Ci_Ci 〇 烧, C3_Ci. a cycloalkyl group, C2_c1 (r alkenyl and C2_Ci〇-alkynyl, wherein the aliphatic or cyclic moiety of the last four groups described above may be unsubstituted, partially or fully halogenated or may have 1 or 2 of the same Or a different substituent Ry, while the other group or the other hydrogen or halogen in rS1, especially hydrogen. More preferably, R4 1 or R5 ! is selected from the group consisting of halogen, CN, c--c4-alkyl, c- C4-haloalkyl, c3-c6-cycloalkyl and c3-c6-halocycloalkyl' and most preferably selected from the group consisting of halogen, CN, Ch3, CH2F, CHF2 and CF3 'simultaneous groups R41 or R51 Further, one is hydrogen. In the formula I and I] of the group A1, the ratio of r6 1 is preferably selected from the group consisting of Cl_Cl〇_alkyl, Cl-C. _haloalkyl, C3-C10-cycloalkyl, (1:3-(310-_-cycloalkyl, c3-C10-cycloalkyl), C3-Ci〇-halocycloalkyl, C2 -C10-alkenyl, c2-cl0_ _ baking base, C1-C4-Hyun-oxy-C^-Cw alkyl, phenyl, benzyl, phenyloxy- fluorenyl, 133661.doc -36- 200917962 5- or 6-shell heteroaryl, 5- or 6-membered heteroarylmethyl, wherein the (hetero)aromatic ring in the last five of the above groups is Substituted or may have 1, 2, 3, 4 or 5 identical or different substituents RX, as defined above and preferably selected from the group consisting of a pectin, c, a c4-alkyl, C]_C4_ Alkyl, Ci_C4_alkoxy, ci&lt;-halogenated 6 oxy, (VC4-alkylsulfonyl and Cl_C4_haloalkylsulfonyl. More preferably c-C4·alkyl or C] _C4_haloalkyl, especially methyl 'ethyl, n-propyl, isopropyl, difluoromethyl, trifluoromethyl, 2-fluoroclay, fluoroethyl and 2,2,2-diethyl Also preferred are those of the A group A1! and „compounds, wherein RSI is as defined herein and wherein R is selected from phenyl, benzyl and 5- or 6-membered heteroaryl, especially 吼Pyridyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl isoxazole, isothiazolyl, 1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl, triazole a 1,2,4-triazolyl or tetrazolyl group in which the aromatic moiety of the phenyl, benzyl and 5- or 6-membered heteroaryl groups is unsubstituted or may have 1, 2 or 3 identical or Different substituents Rx, as defined above and preferably selected from the group consisting of halogen, G-CV leuco, CVCV halogenated alkyl, CrCV Group, burn group, acyl continued CVCV alkyl, halo and C ^ -CU- burning performance acyl group Suitable examples of the group A1-based group of the following formula:. Al a, Al b,

Al.c、Al.d、Al.e、Al.f、Al.g、Al.h、Al.i、Al.k、Al.c, Al.d, Al.e, Al.f, Al.g, Al.h, Al.i, Al.k,

Al.l、Al.m、A1.n、A1_0、Αι·ρ、A1 q、A1 r、M s、Al.l, Al.m, A1.n, A1_0, Αι·ρ, A1 q, A1 r, M s,

Al.t、Al.u、Al.v、Al.w、Al.x、Aly&amp; A1 z,其中 R6i 係 如表A1之一列所定義(基團Ai.al_A1 a81至ai.z1_ Al.z81): 133661.doc -37- 200917962Al.t, Al.u, Al.v, Al.w, Al.x, Aly&amp; A1 z, wherein R6i is as defined in one of the columns of Table A1 (group Ai.al_A1 a81 to ai.z1_ Al.z81) : 133661.doc -37- 200917962

A1.d A1.eA1.d A1.e

,N A1, N A1

m Am A

n 1 An 1 A

NIR 9 T— A #lNIR 9 T- A #l

CHCH

,N 61, N 61

NI6RNI6R

CH p A1CH p A1

,N,N

q 61 NIR A F Hcq 61 NIR A F Hc

,N,N

NIR c A1NIR c A1

c 2 Hc 2 H

(c H((c H(

s A1 u A1s A1 u A1

Kb'/Ryz l H 2 ch3 3 ch2ch3 4 ch2ch2ch3 5 CH(CH3)2 6 ch2cf3 I3366l.doc -38- 200917962 R6I/R52 7 C(CH3)3 8 C6H5 9 4-Cl-C6H4 10 4-F-C6H4 11 2,4-Cl2-C6H3 12 4-(CH30)-C6H4 13 2-0比。定基 14 5 ·氣-2-°比σ定基 15 ch2-c6h5 16 4-(OCF3)-C6H4 17 4-(SCF3)-C6H4 18 4-(OCHF2)-C6H4 19 4-(CF(CF3)2)-C6H4 20 4-(S02CH3)-C6H4 21 2,6-Cl-4-CF3-C6H2 22 3-氣-5-三氟-曱基吼啶-2-基 23 3-吡啶基 24 4-吼咬基 25 2_嗟吐基 26 4,5-二曱基-噻唑-2-基 27 4-α塞α坐基 28 5-°塞σ坐基 29 4-三氟^甲基-嗟〇坐_2·基 30 4-曱基噻唑-2-基 31 4-苯基噻唑-2-基 32 5-三唑基 33 3-曱基-三唑-5-基 34 4-氯苄基 35 4-硝基-1-吡唑基-曱基 36 2-咪唑基 37 4-°米。坐基 38 5-咪α坐基 39 2-°惡咕基 40 4-°惡。坐基 41 5-α惡'•坐基 42 3-異。惡°坐基 43 4-異噁唑基 44 5-異噁唑基 45 3-甲基異噁唑-5-基 46 5-曱基異噁唑-3-基 47 3-°比吐基 133661.doc -39- 200917962 R6i/R52 48 [1,3,4]噻二唑-2-基 49 5-四0坐基 50 4-N02-C6H4 51 4-CF3-C6H4 52 2,4-F2-C6H3 53 3,5-Cl2-C6H3 54 3,4-Cl2-C6H3 55 4-C(CH3)3-C6H4 56 3-Cl-C6H4 57 3-F-C6H4 58 2-F-C6H4 59 2-CF3-C6H4 60 2-CH30-C6H4 61 3-CH30-C6H4 62 3-Cl-4-F-C6H3 63 3-N02-C6H4 64 2-CH3-C6H4 65 3-CH3-C6H4 66 4-CH3-C6H4 67 2-苯基-C6H4 68 3-苯基-C6H4 69 2-F-4-Cl-C6H3 70 2,4,6-Cl3-C6H2 71 2,3,4-Cl3-C6H2 72 2,6-F2-C6H3 73 ch2f 74 chf2 75 cf3 76 ch2chf2 77 ch2ci 78 chci2 79 CC13 80 CH2CHC12 81 ch2cci3 在此處及下表中C6H5表示苯基,CH2-C6H5表示苄基,4-C1-C6H4表示4-氣苯基,4-F-C6H4表示4-氟苯基,4-(CH30)-C6H4表示4-甲氧基苯基,2,4-Cl2-C6H3表示2,4-二氣苯基, 4-(CF(CF3)2)-C6H4表示 4-(1,2,2,2-四氟-1-(三氟甲基)乙基) 苯基,4-(OCF3)-C6H4表示4-(三氟曱氧基)苯基,4-(SCF3)- 133661.doc -40· 200917962 C#4表示4_(三氟曱基硫基)苯基,4-(OCHF2)-C6H4表示4-(二氟曱氧基)苯基,4-(S02CH3)-C6H4表示4_(曱基磺醯基) 笨基’ 2,6-Cl-4-CF3-C6H2表示2,6-二氯-4-(三氟曱基)苯 基,4-NO2-C6H4表不4-硝基苯基,4-CF3-C6H4表示4-(三氣 曱基)苯基,2,4-F2-C6H3 表示 2,4-二氟苯基,3,5-Cl2-C6H3 表示3,5-二氣苯基,3,4-Cl2-C6H3表示3,4-二氯苯基,4-C(CH3)3-C6H4表示4-第三丁基苯基,3-Cl-C6H4表示3-氣苯 基,3-F-C6H4表示3-氟苯基,2-F-C6H4表示2-氟苯基,2-CF3-C6H4表示2-(三氟甲基)苯基,2-CH30-C6H4表示2-曱氧 基苯基,3-CH30-C6H4表示3-曱氧基苯基,3-Cl-4-F-C6H3 表示3-氣-4-氟苯基,3-N02-C6H4表示3-硝基苯基,2-CH3-C6H4表示2-曱苯基,3-CH3-C6H4表示3-甲苯基,4-CH3-C#4表示4-曱苯基,2-苯基-C6H4表示聯苯基2-基,3-笨基_ GH4表示聯笨基3-基,2-F-4-Cl-C6H3表示2-氟-4-氣苯基, 2,4,6-Cl3-C6H2 表示 2,3,4-三氯苯基,2,3,4-Cl3-C6H2 表示 2,3,4-三氣苯基,且2,6-F2-C6H3表示2,6-二氟苯基。 本發明另一實施例係關於式I及II吡唑化合物、其鹽及該 等化合物之方法及應用,其中A係基團A2。其中較佳者係 式I化合物’其中X1、R1、R2及R3係如上文所定義且尤其 具有一種較佳含義。 在其中A係基團A2之式I及II吡唑化合物中,R42較佳係 選自氫、鹵素、CN、CrCV烷基、CVC4-鹵代烷基、Γ C1〇-環炫基、C3_ClQ-鹵代環院基及苯基,其可未經取代&lt; 可具有1、2、3、4或5個相同或不同取代基Rx,其係如上 133661.doc •41 · 200917962 文所定義且其較佳係選自鹵素、C〗_C4_烷基、Ci_c4_自代 烷基、CVC4-烷氧基、代烷氧基、〇1_〇4_烷基磺醯 基、及Cl-C4·鹵代烷基磺醯基。具體而言,R42係選自氫、 鹵素、CN、Cl_c4_烧基、Ci_c4_ _代烧基、c3_C6_環燒基 及CVCV鹵代環烷基,且更佳係選自氫、鹵素、cN、 CH3、CH2F、CHF2及 CF3。 在其中A係基團A2之式I及II吡唑化合物中,R52較佳係 選自由以下組成之群:氫、鹵素、Ci_Ci〇_烷基、C丨_C丨鹵 代烧基、C3_C10-環烧基、C3-C10-鹵代環烧基、C3-C10-環院 基甲基、C3_C10-鹵代環烷基甲基、c2_Ci〇_烯基、 代稀基、CrCV烷氧基_Cl_Cl0_烷基、苯基、苄基、苯氧 基-曱基、5-或6員雜芳基、5_或6員雜芳基曱基,其中上述 最後5個基團中之(雜)芳香族環可未經取代或可具有1、2、 3、4或5個相同或不同取代基RX,其係如上文所定義且較 佳係選自鹵素、(VCV烷基、CVC4-鹵代烷基、Ci_C4_烷氧 基、eve:4-鹵代烷氧基、Ci_C4_烷基磺醯基、及c〗_C4_鹵代 烷基磺醯基。R52更佳係選自由以下組成之蛘:氫、鹵 素、CN、CVC!。-烷基、Cl_C鹵代烷基 ^3-L10- % 烷 基、c3-c10-鹵代環烷基、c3_Ci〇_環烷基甲基、 國代 環烷基甲基、C2_c10-烯基、C2~c10-i代烯基及C〗_C4_烷氧 基烷基。r52更佳係氫、鹵素、Ci_C4_烷基或 鹵代烷基,尤其曱基、乙基、正丙基、異丙基、二氟曱 基、三氟甲基及2,2,2-三氟乙基。同樣較佳者係其中a係基 團A2之式I及II化合物,其中R42及R62係如本 +又所定義且其 133661.doc -42- 200917962 中R52係選自苯基、苄基及5-或6員雜芳基,尤其吼啶基、 吡唑基、咪唑基、噁唑基、噻唑基、異噁唑基、異噻唑 基、1,2,4-噻二唑基、1,3,4-噻二唑基、12,3-三唑基、 1,2,4-三唑基或四唑基,其中笨基、苄基及5_或6員雜芳基 中之芳香族部分未經取代或可具有丨、2或3個相同或不同 取代基Rx,其係如上文所定義且較佳係選自_素、C】_C4_ 烷基、(VCV鹵代烷基、C^CV烷氧基、Cl_c4_鹵代烷氧 基、CrC4-烷基磺醯基、及Cl_c4_鹵代烷基磺醯基。 在其中A係基團A2之式I及π»比。坐化合物中,R62較佳係 選自由以下組成之群:CVCio-烷基、C丨_Cl〇_鹵代烷基' C3-c10-環烷基、c3-c10-i代環烷基、C3_Ci〇_環烷基甲基、 c3-c10-鹵代環烷基曱基、c2_Ci『烯基、c2_Ci〇_鹵代烯基、 C1-C4-烷氧基烷基、笨基、苄基及苯氧基甲基,其 中上述最後3個基團之芳香族環可未經取代或可具有1、 2、3、4或5個相同或不同取代基RX,其係如上文所定義且 更佳係選自鹵素、q-cv烷基、cvc4-鹵代烷基、CVO烷 氧基、G-c:4-鹵代烷氧基、Ci_C4_烷基磺醯基、及Ci_C4_鹵 代烧基績醯基。R62更佳為Ci_C4_烷基或Ci_C4_鹵代烷基, 尤其甲基、乙基、正丙基、異丙基、二氟曱基、三氟曱基 及2,2,2-二氟乙基。 適宜基團A2之實例係以下式之基團:A2.aa、A2.ab、 A2.ac、A2.ad、A2.ae、A2.af、A2.ag、A2.ah、A2.ai、 A2.ak、A2.al、A2.am、A2.an及 A2.ao,其中 R52係如表 A1 之一列所定義(基團 A2.aal-A2.aa81 至 A2.aol-A2.ao81): 133661.doc -43 - 200917962Kb'/Ryz l H 2 ch3 3 ch2ch3 4 ch2ch2ch3 5 CH(CH3)2 6 ch2cf3 I3366l.doc -38- 200917962 R6I/R52 7 C(CH3)3 8 C6H5 9 4-Cl-C6H4 10 4-F-C6H4 11 2,4-Cl2-C6H3 12 4-(CH30)-C6H4 13 2-0 ratio. Stationary 14 5 ·Gas-2-° ratio σ定基15 ch2-c6h5 16 4-(OCF3)-C6H4 17 4-(SCF3)-C6H4 18 4-(OCHF2)-C6H4 19 4-(CF(CF3)2) -C6H4 20 4-(S02CH3)-C6H4 21 2,6-Cl-4-CF3-C6H2 22 3-A-5-trifluoro-indolyl acridine-2-yl 23 3-pyridyl 24 4-bite 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 2·Base 30 4-mercaptothiazol-2-yl 31 4-phenylthiazol-2-yl 32 5-triazolyl 33 3-decyl-triazol-5-yl 34 4-chlorobenzyl 35 4- Nitro-1-pyrazolyl-indenyl 36 2-imidazolyl 37 4-° m. Sit-base 38 5-mi-α sitting base 39 2-° 咕 base 40 4-° evil. Sitting base 41 5-α evil '• sitting base 42 3-iso.恶 ° sita 43 4-isoxazolyl 44 5-isoxazolyl 45 3-methylisoxazole-5-yl 46 5-nonylisoxazole-3-yl 47 3-° ratio 吐 133661 .doc -39- 200917962 R6i/R52 48 [1,3,4]thiadiazole-2-yl 49 5-tetrazole 50 4-N02-C6H4 51 4-CF3-C6H4 52 2,4-F2- C6H3 53 3,5-Cl2-C6H3 54 3,4-Cl2-C6H3 55 4-C(CH3)3-C6H4 56 3-Cl-C6H4 57 3-F-C6H4 58 2-F-C6H4 59 2-CF3- C6H4 60 2-CH30-C6H4 61 3-CH30-C6H4 62 3-Cl-4-F-C6H3 63 3-N02-C6H4 64 2-CH3-C6H4 65 3-CH3-C6H4 66 4-CH3-C6H4 67 2- phenyl-C6H4 68 3-phenyl-C6H4 69 2-F-4-Cl-C6H3 70 2,4,6-Cl3-C6H2 71 2,3,4-Cl3-C6H2 72 2,6-F2-C6H3 73 Ch2f 74 chf2 75 cf3 76 ch2chf2 77 ch2ci 78 chci2 79 CC13 80 CH2CHC12 81 ch2cci3 Here and in the following table, C6H5 represents phenyl, CH2-C6H5 represents benzyl, 4-C1-C6H4 represents 4-phenyl, 4- F-C6H4 represents 4-fluorophenyl, 4-(CH30)-C6H4 represents 4-methoxyphenyl, 2,4-Cl2-C6H3 represents 2,4-diphenyl, 4-(CF(CF3) 2) -C6H4 represents 4-(1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl)phenyl, 4-(OCF3)-C6H4 represents 4-(trifluorodecyloxy) Phenyl, 4-(SC F3)- 133661.doc -40· 200917962 C#4 represents 4_(trifluoromethylthio)phenyl, 4-(OCHF2)-C6H4 represents 4-(difluorodecyloxy)phenyl, 4-(S02CH3 )-C6H4 represents 4_(fluorenylsulfonyl)phenyl] 2,6-Cl-4-CF3-C6H2 represents 2,6-dichloro-4-(trifluoromethyl)phenyl, 4-NO2-C6H4 The table is not 4-nitrophenyl, 4-CF3-C6H4 represents 4-(trimethylsulfonyl)phenyl, 2,4-F2-C6H3 represents 2,4-difluorophenyl, 3,5-Cl2-C6H3 Represents 3,5-diphenylphenyl, 3,4-Cl2-C6H3 represents 3,4-dichlorophenyl, 4-C(CH3)3-C6H4 represents 4-tert-butylphenyl, 3-Cl- C6H4 represents 3-gas phenyl, 3-F-C6H4 represents 3-fluorophenyl, 2-F-C6H4 represents 2-fluorophenyl, 2-CF3-C6H4 represents 2-(trifluoromethyl)phenyl, 2 -CH30-C6H4 represents 2-decyloxyphenyl, 3-CH30-C6H4 represents 3-decyloxyphenyl, 3-Cl-4-F-C6H3 represents 3-vapor-4-fluorophenyl, 3-N02 -C6H4 represents 3-nitrophenyl, 2-CH3-C6H4 represents 2-fluorenylphenyl, 3-CH3-C6H4 represents 3-tolyl, 4-CH3-C#4 represents 4-fluorenylphenyl, 2-phenyl The group -C6H4 represents a biphenyl-2-yl group, the 3-phenyl group _ GH4 represents a phenyl group 3-yl group, and the 2-F-4-Cl-C6H3 represents a 2-fluoro-4-phenyl group, 2, 4, 6 -Cl3-C6H2 represents 2,3,4-trichlorophenyl, 2,3,4-C l3-C6H2 represents 2,3,4-trisylphenyl, and 2,6-F2-C6H3 represents 2,6-difluorophenyl. Another embodiment of the present invention relates to a pyrazole compound of the formula I and II, a salt thereof, and a method and use of the same, wherein the A group A2. Preferred among them are the compounds of the formula I wherein X1, R1, R2 and R3 are as defined above and in particular have a preferred meaning. In the pyrazole compounds of the formula I and II in which the A group A2 is selected, R42 is preferably selected from the group consisting of hydrogen, halogen, CN, CrCV alkyl, CVC4-haloalkyl, ΓC1〇-cyclodyl, C3_ClQ-halogen. Ring-based and phenyl, which may be unsubstituted &lt;1, may have 1, 2, 3, 4 or 5 identical or different substituents Rx, as defined above in 133661.doc • 41 · 200917962 and preferred Is selected from the group consisting of halogen, C _C4_alkyl, Ci_c4_self alkyl, CVC4-alkoxy, alkoxy, 〇1_〇4_alkylsulfonyl, and Cl-C4·haloalkyl sulfonate醯基. Specifically, R42 is selected from the group consisting of hydrogen, halogen, CN, Cl_c4-alkyl, Ci_c4_-alkyl, c3_C6_cycloalkyl, and CVCV halocycloalkyl, and more preferably selected from the group consisting of hydrogen, halogen, cN, CH3, CH2F, CHF2 and CF3. In the pyrazole compounds of the formula I and II in which the A group A2 is present, R52 is preferably selected from the group consisting of hydrogen, halogen, Ci_Ci〇-alkyl, C丨_C丨 haloalkyl, C3_C10- Cycloalkyl, C3-C10-halocycloalkyl, C3-C10-cyclohexylmethyl, C3_C10-halocycloalkylmethyl, c2_Ci〇-alkenyl, substituted dilute, CrCV alkoxy_Cl_Cl0 - alkyl, phenyl, benzyl, phenoxy-indenyl, 5- or 6-membered heteroaryl, 5- or 6-membered heteroaryl fluorenyl, wherein the (hetero) aroma of the last five of the above groups The ethnic ring may be unsubstituted or may have 1, 2, 3, 4 or 5 identical or different substituents RX, as defined above and preferably selected from the group consisting of halogen, (VCV alkyl, CVC4-haloalkyl, Ci_C4_alkoxy, eve: 4-haloalkoxy, Ci_C4_alkylsulfonyl, and c _C4_haloalkylsulfonyl. R52 is more preferably selected from the group consisting of hydrogen, halogen, CN, CVC!--Alkyl, Cl_C haloalkyl^3-L10-% alkyl, c3-c10-halocycloalkyl, c3_Ci〇-cycloalkylmethyl, cycloalkylmethyl, C2_c10-alkenyl , C2~c10-i alkenyl and C _C4_alkoxyalkyl. R52 is better Halogen, Ci_C4_alkyl or haloalkyl, especially decyl, ethyl, n-propyl, isopropyl, difluorodecyl, trifluoromethyl and 2,2,2-trifluoroethyl. Also preferred Is a compound of formula I and II wherein a group A2, wherein R42 and R62 are as defined in the present invention, and wherein R52 is selected from the group consisting of phenyl, benzyl and 5- or 6 in 133661.doc-42-200917962 Heteroaryl, especially acridinyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, 1,2,4-thiadiazolyl, 1,3,4- Thiadiazolyl, 12,3-triazolyl, 1,2,4-triazolyl or tetrazolyl, wherein the aromatic moiety of the stupid, benzyl and 5- or 6-membered heteroaryl is unsubstituted Or may have 丨, 2 or 3 identical or different substituents Rx, as defined above and preferably selected from the group consisting of _, C, _C4_alkyl, (VCV haloalkyl, C^CV alkoxy, Cl_c4 a haloalkoxy group, a CrC4-alkylsulfonyl group, and a Cl_c4_haloalkylsulfonyl group. In the formula I and the π» ratio of the group A group, R62 is preferably selected from the group consisting of Group: CVCio-alkyl, C丨_Cl〇_haloalkyl' C3-c10-cycloalkyl , c3-c10-i cycloalkyl, C3_Ci〇_cycloalkylmethyl, c3-c10-halocycloalkylindenyl, c2_Ci"alkenyl, c2_Ci〇_haloalkenyl, C1-C4-alkane An oxyalkyl group, a benzyl group, a benzyl group and a phenoxymethyl group, wherein the aromatic ring of the last three groups described above may be unsubstituted or may have 1, 2, 3, 4 or 5 identical or different substituents RX, which is as defined above and more preferably selected from the group consisting of halogen, q-cv alkyl, cvc4-haloalkyl, CVO alkoxy, Gc:4-haloalkoxy, Ci_C4-alkylsulfonyl, and Ci_C4 _ halogenated base. R62 is more preferably Ci_C4_alkyl or Ci_C4_haloalkyl, especially methyl, ethyl, n-propyl, isopropyl, difluorodecyl, trifluoromethyl and 2,2,2-difluoroethyl. Examples of suitable groups A2 are those of the formula: A2.aa, A2.ab, A2.ac, A2.ad, A2.ae, A2.af, A2.ag, A2.ah, A2.ai, A2 .ak, A2.al, A2.am, A2.an and A2.ao, where R52 is as defined in one of the tables in Table A1 (group A2.aal-A2.aa81 to A2.aol-A2.ao81): 133661 .doc -43 - 200917962

R 52R 52

R 52R 52

CH3 R 52 ch2f r 52 chf2 r 52CH3 R 52 ch2f r 52 chf2 r 52

CF 3 、N,# 、N’ # IM、厂 N H H H H H A2.aa A2.ab A2.ac A2.ad A2.ae 、# 、52 52 52 A2.ao A2.ai A2.am A2.an 適宜基團A2之其他實例係以下式之基團:A2.ba、 A2.bb、A2.be、A2.bd、A2.be、A2.bf、A2.bg、A2.bh、 A2.bi、A2.bk、A2.bl、A2.bm、A2.bn及 A2.bo,其中 R52係 如表A1之一列所定義(基團A2.bal-A2.ba81至A2.bol-A2.bo81):CF 3 , N, # , N' # IM, plant NHHHHH A2.aa A2.ab A2.ac A2.ad A2.ae , # , 52 52 52 A2.ao A2.ai A2.am A2.an Suitable group Other examples of A2 are groups of the formula: A2.ba, A2.bb, A2.be, A2.bd, A2.be, A2.bf, A2.bg, A2.bh, A2.bi, A2.bk , A2.bl, A2.bm, A2.bn and A2.bo, where R52 is as defined in the column A1 (group A2.bal-A2.ba81 to A2.bol-A2.bo81):

# A2.af# A2.af

Cl R 、#Cl R,#

Br 、#Br,#

I R #I R #

CN N、 、# A2.ag A2.ah R5\ CH2CH3 R5\ (CH2)2CH3 r\ N、 、# N、 '# N、 A2.ai CH(CH3)2 、# A2.akCN N, , # A2.ag A2.ah R5\ CH2CH3 R5\ (CH2)2CH3 r\ N, , # N, '# N, A2.ai CH(CH3)2 , # A2.ak

HH

R 52 N、 I ch3 A2.baR 52 N, I ch3 A2.ba

# 、52 ch2f r N I ch3 A2.be '# 52# 、52 ch2f r N I ch3 A2.be '# 52

N 、# I ch3 A2.bdN, # I ch3 A2.bd

# A2.be# A2.be

A2.bfA2.bf

A2.bh A2_bi A2_bk 133661.doc -44 - 200917962A2.bh A2_bi A2_bk 133661.doc -44 - 200917962

CH 3CH 3

CH 3CH 3

CH 3 A2.bl A2.bm A2.bn A2.bo 。 適宜基團A2之其他實例係以下式之基團:A2.ca、 A2.cb、A2.cc、A2.cd、A2.ce、A2.cf、A2.cg、A2.ch、 A2.ci、A2.ck、A2.cl、A2.cm、A2.cn及 A2.co,其中 R52係 如表A1之一列所定義(基團A2.cal-A2.ca81至A2.col-A2.co8 1): 52CH 3 A2.bl A2.bm A2.bn A2.bo . Other examples of suitable groups A2 are those of the formula: A2.ca, A2.cb, A2.cc, A2.cd, A2.ce, A2.cf, A2.cg, A2.ch, A2.ci, A2.ck, A2.cl, A2.cm, A2.cn and A2.co, wherein R52 is as defined in one of the columns of Table A1 (group A2.cal-A2.ca81 to A2.col-A2.co8 1) : 52

R # A2.ca Ν' N I CHF. CH, '#R # A2.ca Ν' N I CHF. CH, '#

A2.cc A2.cd A2.ce 2 A2.cbA2.cc A2.cd A2.ce 2 A2.cb

A2.cg A2.ch A2.ci A2.ck A2.cfA2.cg A2.ch A2.ci A2.ck A2.cf

,52 CHF2 A2.cm N、, 52 CHF2 A2.cm N,

N I CHF A2.cn ch(ch3)2 #N I CHF A2.cn ch(ch3)2 #

適宜基團A2之其他實例係以下式之基團:A2.da、 A2.db、A2.dc、A2.dd、A2.de、A2.df、A2.dg、A2.dh、 A2.di、A2.dk、A2.dl、A2.dm、A2.dn及 A2.do,其中 R52係 133661.doc -45- 200917962 如表A1之一列所定義(基團A2_dal-A2.da81至A2.dol· A2.do81):Other examples of suitable groups A2 are those of the formula: A2.da, A2.db, A2.dc, A2.dd, A2.de, A2.df, A2.dg, A2.dh, A2.di, A2.dk, A2.dl, A2.dm, A2.dn and A2.do, where R52 is 133661.doc -45- 200917962 as defined in one of the tables A1 (group A2_dal-A2.da81 to A2.dol· A2.do81):

52 ch2ch3 r 52 (CH2)2CH3 R 5252 ch2ch3 r 52 (CH2)2CH3 R 52

A2.dA2.d

I CF3 A2.dkI CF3 A2.dk

R N、 N I CF, '# Ν' A2.dl 'N I cf3 A2.dm '# N、, N I cf3 A2.dn '# (ch(ch3)2 rR N, N I CF, '# Ν' A2.dl 'N I cf3 A2.dm '# N,, N I cf3 A2.dn '# (ch(ch3)2 r

A2.d〇 v.. 本發明另一實施例係關於式I及II °比°坐化合物、其鹽及. 等化合物之方法及應用,其中A係基團A3。其中較佳者 式I化•合物,其中X1、R〗、R2及R3係如上文所定義且尤 具有一種較佳含義。 在其中A係基團A3之式I及II吡唑化合物中,R43較佳 選自氫、鹵素、CN、(VCV烷基、CVCV鹵代烷基、c C10-if&lt;烷基、C3-C1G-鹵代環烷基及苯基,其可未經取代 可具有1、2、3、4或5個相同或不同取代基RX,其係如 文所定義且其較佳係選自鹵素、Ci_C4_烷基、Ci_Cp鹵 133661 .doc -46 · 200917962 烷基Cl-C4_烷氧基、CVC4·鹵代烷氧基、Cl_C4_烷基磺醯 基及C1-C4_鹵代烷基磺醯基《具體而言,R43係選自氫、 函素CN、Ci-CV烧基、CVC4-函代烷基、c3-C6-環烷基 及C3_CV鹵代環烷基,且較佳選自氫、鹵素、、cH3、 CH2F、CHF2及 cf3。A2.d〇 v.. Another embodiment of the present invention relates to a method and application of a compound such as a compound of the formula I and II °, a salt thereof, and the like, wherein the group A is A3. Among them, preferred are the compounds of the formula I, wherein X1, R, R2 and R3 are as defined above and have a preferred meaning. In the pyrazole compounds of the formula I and II wherein the group A is A, R43 is preferably selected from the group consisting of hydrogen, halogen, CN, (VCV alkyl, CVCV haloalkyl, c C10-if &lt; alkyl, C3-C1G-halogen Cycloalkyl and phenyl, which may be unsubstituted, may have 1, 2, 3, 4 or 5 identical or different substituents RX, as defined herein and preferably selected from halogen, Ci_C4-alkane. Base, Ci_Cp halide 133661 .doc -46 · 200917962 Alkyl Cl-C4_alkoxy, CVC4.haloalkoxy, Cl_C4_alkylsulfonyl and C1-C4_haloalkylsulfonyl" Specifically, R43 It is selected from the group consisting of hydrogen, a nutrient CN, a Ci-CV alkyl group, a CVC4-complex alkyl group, a c3-C6-cycloalkyl group, and a C3_CV halocycloalkyl group, and is preferably selected from the group consisting of hydrogen, halogen, cH3, CH2F. , CHF2 and cf3.

在其中A係基團A3之式吡唑化合物中,R53較佳係 避自由以下組成之群:氫、_素、c,-c】0-烷基、c】-c丨〇-鹵 代烷基、C3-C1G-環烷基、代環烷基、C3_CiQ-環烷 基甲基、c3-c〗“代環烷基甲基、c2_Ci。-烯基、c2_c】。__ 代烯基、Ci-CV烷氧基-CVCw烷基、苯基、苄基、笨氧 基-甲基、5-或6員雜芳基、5-或6員雜芳基甲基,其中上述 最後5個基團中之(雜)芳香族環可未經取代或可具有1、2、 、4或5個相同或不同取代基RX,其係如上文所定義且較 佳係選自鹵素、Ci-CV烷基、CVCU-鹵代烷基、Ci_c4_烷氧 基、CVC4-函代炫氧基、Cl_c4_院基確酿基、及Ci_c4_齒代 烷基磺醯基。R53更佳係選自由以下組成之群:氫 '鹵 素、CN、(:!-(:!〇-烷基、CVCw鹵代烷基、c ^3-Lio-被烧 基、C3-C10-ii代環烷基、C3-C丨〇-環烷基甲基 丞 L3-C10-鹵代In the pyrazole compound of the formula A3, R53 is preferably free from the group consisting of hydrogen, _, c, -c] 0-alkyl, c]-c丨〇-haloalkyl, C3-C1G-cycloalkyl, cycloalkyl, C3_CiQ-cycloalkylmethyl, c3-c "cycloalkylmethyl, c2_Ci.-alkenyl, c2_c].__ alkenyl, Ci-CV alkoxy-CVCw alkyl, phenyl, benzyl, phenoxy-methyl, 5- or 6-membered heteroaryl, 5- or 6-membered heteroarylmethyl, wherein the last five of the above groups The (hetero)aromatic ring may be unsubstituted or may have 1, 2, 4 or 5 identical or different substituents RX, as defined above and preferably selected from halogen, Ci-CV alkyl, CVCU a haloalkyl group, a Ci_c4_alkoxy group, a CVC4-comonyloxy group, a Cl_c4_institutional group, and a Ci_c4_dentate alkylsulfonyl group. R53 is more preferably selected from the group consisting of hydrogen' Halogen, CN, (:!-(:!〇-alkyl, CVCw haloalkyl, c^3-Lio-alkyl, C3-C10-ii cycloalkyl, C3-C丨〇-cycloalkyl Based on L3-C10-halogenated

環烷基甲基、C2-C10-烯基、C2_C10-鹵代烯基及C〗_C4_烷氧 基- Ci-Ci〇-炫基。R更佳係氣、鹵素' 義戍c C 鹵代烧基’尤其甲基、乙基、正丙基、展屯 升内基、二氟曱 基、二乱曱基或2,2,2 -二敗乙基。同樣較佳者係其中其^ 團A2之式I及II化合物,其中R43及R63係如太— ’'土 *又所定義且其 中R53係選自苯基、苄基及5-或6員雜芳基, 、 凡其吼咬基、 133661.doc •47- 200917962 吡唑基、咪唑基、噁唑基、噻唑基、異噁唑基、異噻唑 基、1,2,4-噻二唑基、:ι,3,4-噻二唑基、^夂三唑基、 1,2,4-三唑基或四唑基,其中苯基、苄基及5_或6員雜芳基 中之芳香族部分未經取代或可具有丨、2或3個相同或不同 取代基R,其係如上文所定義且較佳係選自鹵素、 烷基、CrCV齒代烷基、Cl_C4_烷氧基、Ci_C4_ _代烷氧 基、G-C4·烷基磺醯基、及Ci_C4_鹵代烷基磺醯基。 在其中A係基團A3之式I及π。比唑化合物中,R63較佳係 選自由以下組成之群··氫、Ci_Ci〇_烧基、Ci_Ci〇_齒代烷 基、c3-c10-環烷基、代環烷基、C3_c『環烷基甲 基、c3-Cl『函代環烧基曱基、C2_Ci〇.稀基、C2_Ci“代烯 基、CVCr烷氧基-cVC〗〇_烷基、苯基、苄基、苯氧基-甲 基、5-或6員雜芳基、5_或6員雜芳基甲基,其中上述最後$ 個基團中之(雜)芳香族環可未經取代或可具有丨、2、3、4 或5個相同或不同取代基RX,其係如上文所定義且較佳係 選自鹵素、CVC4-院基、Ci_C4_鹵代烷基、Ci_C4_烧氧基、Cycloalkylmethyl, C2-C10-alkenyl, C2_C10-haloalkenyl and C _C4_alkoxy-Ci-Ci fluorenyl. R is better gas, halogen ' 戍 c C halogenated alkyl', especially methyl, ethyl, n-propyl, fluorene, difluoroindenyl, diterpenoid or 2,2,2 - Two defeated ethyl. Also preferred are compounds of the formulae I and II wherein R.sup.43 and R.sup.6 are as defined above, and wherein R.sup.5 is selected from the group consisting of phenyl, benzyl and 5- or 6-membered. Aryl, aryl, 133661.doc •47- 200917962 pyrazolyl, imidazolyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, 1,2,4-thiadiazolyl ,: i, 3,4-thiadiazolyl, trioxazolyl, 1,2,4-triazolyl or tetrazolyl, of which phenyl, benzyl and 5- or 6-membered heteroaryl The aromatic moiety is unsubstituted or may have fluorene, 2 or 3 identical or different substituents R, as defined above and preferably selected from the group consisting of halogen, alkyl, CrCV dentate alkyl, Cl_C4_alkoxy , Ci_C4__alkoxy, G-C4.alkylsulfonyl, and Ci_C4_haloalkylsulfonyl. In the formula I, the group A and the π. In the azole compound, R63 is preferably selected from the group consisting of hydrogen, Ci_Ci〇-alkyl, Ci_Ci〇_dentylalkyl, c3-c10-cycloalkyl, cycloalkyl, C3_c "cycloalkane" Methyl, c3-Cl "complex cycloalkyl", C2_Ci〇. dilute, C2_Ci "alkenyl, CVCr alkoxy-cVC" 烷基-alkyl, phenyl, benzyl, phenoxy- a methyl, 5- or 6-membered heteroaryl, 5- or 6-membered heteroarylmethyl group, wherein the (hetero)aromatic ring in the last of the above groups may be unsubstituted or may have hydrazine, 2, 3 , 4 or 5 identical or different substituents RX, as defined above and preferably selected from the group consisting of halogen, CVC4-hospital, Ci_C4_haloalkyl, Ci_C4_alkoxy,

Ci c4 i代烧氧基、燒基續醯基、及Ci_C4_鹵代燒基 磺醯基。R53更佳係C|_C4_烷基或Ci_C4_鹵代烷基,尤其甲 基、乙基、正丙基、異丙基、二氟甲基、三氟甲基及 2,2,2-三氟乙基。同樣較佳者係其中a係基團a2之式丨及工】 化口物其中R及R 3係如本文所定義且其中R53係選自苯 基、节基及5_或6員雜芳基’尤其吼咬基、。比咏基、咪唑 基、噁唑基、噻唑基、異噁唑基、異噻唑基、1,2,4-噻二 峻基、坐基、1,2,3-三。坐基、1,2,4-三。坐基或四 133661.doc •48· 200917962 唑基,其中苯基、苄基及5 -或6員雜芳基之芳香族部分未 經取代或可具有1、2或3個相同或不同取代基Rx,其係如 上文所定義且較佳係選自鹵素、q-C4-烷基、C^-CU-鹵代 烷基、CVC4-烷氧基、CVC4-鹵代烷氧基、cvc4-炫基磺醯 基、及鹵代烷基磺醯基。 在其中A係基團A3之式I及IID比峻化合物中,尤佳者係其 中R5或R63係氫、CN、(^-(^-烧基或CrCV鹵代烧基(尤其 氫、CN、CH3、CH2F、CHF2或CF3)之彼等,其中R53亦可 為鹵素,同時R53、R03之另一基團係選自由以下組成之 群:烷基、eve,鹵代烷基、C3-C10-環烷基、c3-c10- |g代環院基、c3-Ci〇-環烷基甲基、C3-C10- _代環烷基 甲基、C2-C10-烯基、C2-C10-i代烯基、CVCV院氧基-C,-c10-烷基、苯基、苄基、苯氧基-曱基、5_或6員雜芳基、 5 -或6員雜芳基甲基,其中上述最後5個基團中之(雜)芳香 族環可未經取代或可具有1、2、3、4或5個相同或不同取 代基Rx ’其係如上文所定義且尤其係選自鹵素、C]C4烷 基、CVC4-鹵代烷基、q-CV烷氧基、(VCV鹵代烷氧基、 C1-C4-烷基績醯基、及c^CV鹵代烷基續醯基。 具體而言R63係氫、CN、Cl-C4-烷基或烷基, 尤其虱、CN、CH3、CH2F、CHF2 或 CF3,且 R53 係選自 c,· C:4·烧基、C〗-C4_鹵代烷基’尤其甲基、乙基、正丙基、異 丙基、二氟甲基、三氟甲基及2,2,2-三氟乙基、苯基、节 基及5 -或6員雜芳基’尤其吡啶基、吡唑基、_。坐基、嗔 &quot;坐基、噻唑基、異噁唑基、異噻唑基、丨,2,4_噻二唑基、 133661 .doc -49- 200917962 1,3,4-噻二唑基、ι,2,3-三唑基、1,2,4-三唑基或四唑基, 其中苯基、苄基及5-或6員雜芳基中之芳香族部分未經取 代或了具有1、2或3個相同或不同取代基rx,其係如上文 所疋義且較佳係選自鹵素、Ci-CU-烧基、鹵代烧 基、cvcv烷氧基、cvc4-鹵代烷氧基、cvc4-烷基磺醯 基、及C〗-C4_鹵代烷基磺醯基, 或 R53係氫、鹵素、CN、CVC4-烷基或cvc4-鹵代烷基,尤 其氫、CN、CH3、CH2F、CHF2或 CF3,且 R63係選自 C|-C4_ 烧基、Ci-C:4-鹵代烷,尤其曱基、乙基、正丙基、異丙 基、二氟曱基、三氟甲基及2,2,2-三氟乙基、苯基、苄基 及5 -或6員雜芳基’尤其。比咬基、吼唾基、咪嗤基、嗯。坐 基、噻唑基、異噁唑基、異噻唑基、1,2,4_噻二唑基' 1,3,4-噻二唑基、丨,2,3_三唑基、丨义仁三唑基或四唑基, 其中苯基、苄基及5-或6員雜芳基中之芳香族部分未經取 代或可具有1、2或3個相同或不同取代基rx,其係如上文 所疋義且較佳係選自鹵素、C丨-C4·烧基、c〗-C4-_代烧 基、Ci-CV烷氧基、CVC4-鹵代烷氧基、c]-c4-烷基磺醯 基鹵代烧基續酿基。 適宜基團A3之實例係以下式之基團:A3.aa、A3.ab、 A3.ac、A3.ad、A3.ae、A3 af、A3 ag、A3 ah、A3 y、 八341^、八3.31、八3.3111、八3』11及八3』〇,其中1^63係如表八3 之一列所定義(基團八3.&amp;&amp;1-入3】81至入3,3〇1-入3.3〇81): 133661.doc •50- 200917962Ci c4 i is an alkoxy group, a decyl group, and a Ci_C4_haloalkylsulfonyl group. R53 is more preferably C|_C4_alkyl or Ci_C4_haloalkyl, especially methyl, ethyl, n-propyl, isopropyl, difluoromethyl, trifluoromethyl and 2,2,2-trifluoroethyl base. Also preferred are those in which the a group a2 is a compound wherein R and R 3 are as defined herein and wherein R53 is selected from phenyl, benzyl and 5- or 6-membered heteroaryl. 'Especially bite base. Specific thiol, imidazolyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, 1,2,4-thiadithio, sylylene, 1,2,3-tri. Sitting base, 1, 2, 4-three. Sodium or 133661.doc •48· 200917962 Azolyl, wherein the aromatic moiety of the phenyl, benzyl and 5- or 6-membered heteroaryl is unsubstituted or may have 1, 2 or 3 identical or different substituents Rx, which is as defined above and preferably selected from the group consisting of halogen, q-C4-alkyl, C^-CU-haloalkyl, CVC4-alkoxy, CVC4-haloalkoxy, cvc4-nonylsulfonyl And haloalkylsulfonyl. Among the formula I and the IID of the A group A3, it is preferred that R5 or R63 is hydrogen, CN, (^-(^-alkyl or CrCV halogenated alkyl (especially hydrogen, CN, And CH3, CH2F, CHF2 or CF3), wherein R53 may also be halogen, and the other group of R53, R03 is selected from the group consisting of alkyl, eve, haloalkyl, C3-C10-cycloalkane , c3-c10- |g substituted ring, c3-Ci〇-cycloalkylmethyl, C3-C10- _cycloalkylmethyl, C2-C10-alkenyl, C2-C10-i , CVCV, oxy-C, -c10-alkyl, phenyl, benzyl, phenoxy-indenyl, 5- or 6-membered heteroaryl, 5- or 6-membered heteroarylmethyl, wherein The (hetero)aromatic ring in the last 5 groups may be unsubstituted or may have 1, 2, 3, 4 or 5 identical or different substituents Rx ', as defined above and especially selected from halogen, C] C4 alkyl, CVC 4-haloalkyl, q-CV alkoxy, (VCV haloalkoxy, C1-C4-alkyl fluorenyl, and c^CV haloalkyl fluorenyl. Specifically R63 hydrogen , CN, Cl-C4-alkyl or alkyl, especially hydrazine, CN, CH3, CH2F, CHF2 or CF3, and R53 is selected from c, C:4·alkyl, C--C4_haloalkyl' especially methyl, ethyl, n-propyl, isopropyl, difluoromethyl, trifluoromethyl and 2,2,2-trifluoroethyl , phenyl, benzyl and 5- or 6-membered heteroaryl 'especially pyridyl, pyrazolyl, y. succinyl, 嗔&quot; succinyl, thiazolyl, isoxazolyl, isothiazolyl, anthracene, 2 , 4_thiadiazolyl, 133661 .doc -49- 200917962 1,3,4-thiadiazolyl, iota, 2,3-triazolyl, 1,2,4-triazolyl or tetrazolyl, Wherein the aromatic moiety of the phenyl, benzyl and 5- or 6-membered heteroaryl is unsubstituted or has 1, 2 or 3 identical or different substituents rx, as defined above and preferably Selected from halogen, Ci-CU-alkyl, halogenated alkyl, cvcv alkoxy, cvc4-haloalkoxy, cvc4-alkylsulfonyl, and C-C4-haloalkylsulfonyl, or R53 Hydrogen, halogen, CN, CVC4-alkyl or cvc4-haloalkyl, especially hydrogen, CN, CH3, CH2F, CHF2 or CF3, and R63 is selected from C|-C4_alkyl, Ci-C: 4-haloalkane, especially Sulfhydryl, ethyl, n-propyl, isopropyl, difluorodecyl, trifluoromethyl and 2,2,2-trifluoroethyl, phenyl, And 5- or 6-membered heteroaryl 'especially. Than base, oxime, imidin, um. succinyl, thiazolyl, isoxazolyl, isothiazolyl, 1,2,4 thiadipine Azolyl ' 1,3,4-thiadiazolyl, anthracene, 2,3-triazolyl, oxime triazole or tetrazolyl, wherein phenyl, benzyl and 5- or 6-membered heteroaryl The aromatic moiety in the unsubstituted or may have 1, 2 or 3 identical or different substituents rx, as defined above and preferably selected from the group consisting of halogen, C丨-C4·alkyl, c- C4-_alkylene, Ci-CV alkoxy, CVC4-haloalkoxy, c]-c4-alkylsulfonylhalocarboyl. Examples of suitable groups A3 are those of the formula: A3.aa, A3.ab, A3.ac, A3.ad, A3.ae, A3 af, A3 ag, A3 ah, A3 y, eight 341^, eight 3.31, eight 3.3111, eight 3′′ 11 and eight 3′′〇, of which 1^63 is as defined in one of the tables in Table 8 (Group 8 3.&amp;&amp;1-in 3]81 to 3,3〇 1-in 3.3〇81): 133661.doc •50- 200917962

3 6 N—R3 6 N-R

A3.aa A3.ab A3.ac A3.ad A3.ae CH3CH2 # CH3(CH2)2 # (CH3)2CH # # NC #A3.aa A3.ab A3.ac A3.ad A3.ae CH3CH2 # CH3(CH2)2 # (CH3)2CH # # NC #

3 6 NIR3 6 NIR

、N, N

NIRNIR

'N'N

'N'N

3 ,6 NIR3,6 NIR

VAXVAX

3 6 NIR3 6 NIR

'N'N

N A3.akN A3.ak

3 6 NIR A3.af A3.ag A3.ah A3_ai # cl #3 6 NIR A3.af A3.ag A3.ah A3_ai # cl #

Br # # WR63Br # # WR63

、N, N

3 • 6 NIR3 • 6 NIR

3 6 NIR3 6 NIR

广NI63R A3.al A3.am A3.an A3.ao 。 表A3 : W 1 H 2 ch3 3 ch2ch3 4 ch2ch2ch3 5 ch(ch3)2 6 ch2cf3 7 C(CH3)3 8 c6h5 9 4-Cl-C6H4 10 4-F-C6H4 11 2,4-Cl2-C6H3 12 4-(CH30)-C6H4 13 2-0比变基 14 5-氣-2·β比ΰ定基 15 ch2-c6h5 16 4-(〇CF3)-C6H4 17 4-(SCF3)-C6H4 18 4-(OCHF2)-C6H4 19 4-(CF(CF3)2)-C6H4 20 4-(S02CH3)-C6H4 133661.doc -51 - 200917962 21 2,6-Cl-4-CF3-C6H2 22 3·鼠-5-二氣-甲基0比嗔-2-基 23 3-吡啶基 24 4-0比°定基 25 2-嗔α坐基 26 4,5-二甲基-噻唑-2-基 27 斗-嗟座基 28 5-噻唑基 29 4-三氟甲基-噻唑-2-基 30 4-曱基噻唑-2-基 31 4-苯基噻唑-2-基 32 5-三唑基 33 3-曱基-三唑-5-基 34 4-氣苄基 35 4-硝基-1-。比唑基-曱基 36 2-咪唑基 37 4-°米峻基 38 5-味。坐基 39 2-°惡吐基 40 4-。惡吐基 41 坐基 42 3-異噁唑基 43 4-異噁峻基 44 5-異噁。坐基 45 3-曱基異噁唑-5-基 46 5-曱基異噁唑-3-基 47 3-0比σ坐基 48 [1,3,4]噻二唑-2-基 49 5-四°坐基 50 4-N02-C6H4 51 4-CF3-C6H4 52 2,4-F2-C6H3 53 3,5-Cl2-C6H3 54 3,4-Cl2-C6H3 55 4-C(CH3)3-C0H4 56 3-Cl-C6H4 57 3-F-C6H4 58 2-F-C6H4 59 2-CF3-C6H4 60 2-CH30-C6H4 61 3-CH30-C6H4 133661.doc -52- 200917962 R53/Rw 62 3_Cl-4-F-C6H3 63 3-N〇2-C6H4 64 2-CH3-C6H4 65 3-CH3-QH4 66 4-CH3-C6H4 67 2-苯基-C6H4 68 3-苯基-C6H4 69 2-F-4-Cl-C6H3 70 2,4,6-Cl3-C6H2 71 2,3,4-Cl3-C6H2 72 2,6-F2-C6H3 73 ch2f 74 chf2 75 cf3 76 ch2chf2 77 ch2ci 78 CHC12 79 CC13 80 CH2CHC12 81 CH2CC13 適宜基團A3之其他實例係以下式之基團:A3.ba、 A3.bb、A3.bc、A3.bd、A3.be、A3.bf、A3.bg、A3.bh、 八3.1^、八3上1&lt;;、八3.1)1、八3.1)]11、八3.1)11及八3.1)〇,其中1163係 如表A3之一列所定義(基團A3.bal-A3.ba81至A3.bol-A3.bo81): c O H # clWide NI63R A3.al A3.am A3.an A3.ao. Table A3: W 1 H 2 ch3 3 ch2ch3 4 ch2ch2ch3 5 ch(ch3)2 6 ch2cf3 7 C(CH3)3 8 c6h5 9 4-Cl-C6H4 10 4-F-C6H4 11 2,4-Cl2-C6H3 12 4 -(CH30)-C6H4 13 2-0 ratio mutated 14 5-gas-2·β specific thiol group 15 ch2-c6h5 16 4-(〇CF3)-C6H4 17 4-(SCF3)-C6H4 18 4-(OCHF2 )-C6H4 19 4-(CF(CF3)2)-C6H4 20 4-(S02CH3)-C6H4 133661.doc -51 - 200917962 21 2,6-Cl-4-CF3-C6H2 22 3·rat-5-two Gas-methyl 0 is more than 嗔-2-yl 23 3-pyridyl 24 4-0 ratio ° 25 2-嗔α-based 26 4,5-dimethyl-thiazol-2-yl 27 bucket-嗟 base 28 5-thiazolyl 29 4-trifluoromethyl-thiazol-2-yl 30 4-mercaptothiazol-2-yl 31 4-phenylthiazol-2-yl 32 5-triazolyl 33 3-fluorenyl- Triazol-5-yl 34 4-sulfobenzyl 35 4-nitro-1-. Bizozolyl-fluorenyl 36 2-imidazolyl 37 4-° Mickey 38 5-flavor. Sit-base 39 2-° oxazepine 40 4-. Oxypyrazine 41 Sitrate 42 3-Isooxazolyl 43 4-isoxyl group 44 5-isor. Sitrate 45 3-mercaptoisoxazole-5-yl 46 5-mercaptooxazol-3-yl 47 3-0 σ sylylene 48 [1,3,4]thiadiazol-2-yl 49 5-four° sitting base 50 4-N02-C6H4 51 4-CF3-C6H4 52 2,4-F2-C6H3 53 3,5-Cl2-C6H3 54 3,4-Cl2-C6H3 55 4-C(CH3)3 -C0H4 56 3-Cl-C6H4 57 3-F-C6H4 58 2-F-C6H4 59 2-CF3-C6H4 60 2-CH30-C6H4 61 3-CH30-C6H4 133661.doc -52- 200917962 R53/Rw 62 3_Cl -4-F-C6H3 63 3-N〇2-C6H4 64 2-CH3-C6H4 65 3-CH3-QH4 66 4-CH3-C6H4 67 2-Phenyl-C6H4 68 3-Phenyl-C6H4 69 2-F -4-Cl-C6H3 70 2,4,6-Cl3-C6H2 71 2,3,4-Cl3-C6H2 72 2,6-F2-C6H3 73 ch2f 74 chf2 75 cf3 76 ch2chf2 77 ch2ci 78 CHC12 79 CC13 80 CH2CHC12 81 CH2CC13 Other examples of suitable groups A3 are those of the formula: A3.ba, A3.bb, A3.bc, A3.bd, A3.be, A3.bf, A3.bg, A3.bh, eight3.1 ^, 八三上1&lt;;, eight 3.1) 1, eight 3.1)] 11, eight 3.1) 11 and eight 3.1) 〇, of which 1163 is as defined in one of the tables A3 (group A3.bal-A3.ba81 To A3.bol-A3.bo81): c OH # cl

、N, N

3 *6 NIR a3 *6 NIR a

、N #, N #

c 0 H Fc 0 H F

3 6 NIR a3 6 NIR a

,N #, N #

c Hc H

3 &gt;6 NIR Λ - a # c o3 &gt;6 NIR Λ - a # c o

3 6 NIR a3 6 NIR a

'N #'N #

3 6 NIR A3.bb A3.be A3.be A3.ba3 6 NIR A3.bb A3.be A3.be A3.ba

CH3(CH2)2 # (CH3)2CH A3.bfCH3(CH2)2 # (CH3)2CH A3.bf

ClCl

,N,N

N 63 R A3.bgN 63 R A3.bg

Cl·Cl·

3 6 NIR3 6 NIR

A3.bd # 、NA3.bd #, N

c N A3.bh A3.bi A3.bk a n/i63r # 133661.doc -53 200917962c N A3.bh A3.bi A3.bk a n/i63r # 133661.doc -53 200917962

# A3.bo / 適宜基團A3之其他實例係以下式之基團:A3.ca、 A3.cb、A3.cc、A3.cd、A3.ce、A3.cf、A3.cg、A3.ch、 A3.ci、A3.ck、A3.cl、A3.cm、A3.cn及 A3.co,其中 R53係 如表A3之一歹ij所定義(基團A3.cal-A3.ca81至A3.col-A3.co81):# A3.bo / Other examples of suitable groups A3 are groups of the formula: A3.ca, A3.cb, A3.cc, A3.cd, A3.ce, A3.cf, A3.cg, A3.ch , A3.ci, A3.ck, A3.cl, A3.cm, A3.cn and A3.co, wherein R53 is as defined in one of Table A3, 歹ij (group A3.cal-A3.ca81 to A3. col-A3.co81):

##

CH,CH. # CHJCH丄 # (CH丄CHCH, CH. # CHJCH丄 # (CH丄CH

A3.cf A3, eg A3.ehA3.cf A3, eg A3.eh

/N/N

##

RR

H A3, clH A3, cl

A3.cmA3.cm

A3.cnA3.cn

r53^^ /N R N H A3, co 適宜基團A3之其他實例係以下式之基團:A3.da、 A3.db、A3.de、A3.dd、A3.de、A3.df、A3.dg、A3.dh、 八3.以、八3.(11^、八3.(1卜八3.4111、八3,(111及八3,£1〇其中尺53係如 表A3之一列所定義(基團A3.dal-A3.da81至A3.dol- 133661.doc -54- 200917962 A3.do81):R53^^ /NRNH A3, co Other examples of suitable groups A3 are groups of the formula: A3.da, A3.db, A3.de, A3.dd, A3.de, A3.df, A3.dg, A3.dh, 八三.以,八三.(11^,八三.(1卜八3.4111,八三,(111 and 八3, £1〇) The rule 53 is as defined in one of the tables in Table A3. Mission A3.dal-A3.da81 to A3.dol- 133661.doc -54- 200917962 A3.do81):

A3.daA3.da

# FH2C # F2HC, R 53# FH2C # F2HC, R 53

./N N I ch3 A3.dc./N N I ch3 A3.dc

R 5:R 5:

,N 、NT I ch3 A3.dd, N, NT I ch3 A3.dd

##

CH3CH2 # CH3(CH2)? # (CH3)2CH.NCH3CH2 # CH3(CH2)? # (CH3)2CH.N

R 53R 53

N I CH3 A3.df R N I ch3 A3.dgN I CH3 A3.df R N I ch3 A3.dg

R 53R 53

# N I CH,# N I CH,

A3.diA3.di

# NC# NC

# A3.dh# A3.dh

適宜基團A3之其他實例係以下式之基團:A3.ea、 A3.eb、A3.ec、A3.ed、A3.ee、A3.ef、A3.eg、A3.eh、 A3.ei、A3.ek、A3.el、A3.em、A3.en及 A3.eo,其中 R53係 如表A3之一列所定義(基團A3.eal-A3.ea81至A3.eol-A3.eo81):Other examples of suitable groups A3 are those of the formula: A3.ea, A3.eb, A3.ec, A3.ed, A3.ee, A3.ef, A3.eg, A3.eh, A3.ei, A3.ek, A3.el, A3.em, A3.en and A3.eo, wherein R53 is as defined in one of the tables A3 (group A3.eal-A3.ea81 to A3.eol-A3.eo81):

A3.ea A3.ebA3.ea A3.eb

A3.ecA3.ec

A3.ed A3.ee 133661.doc -55- 200917962 ch3ch2 # CH3(CH2)2 # (CH3)2CH,A3.ed A3.ee 133661.doc -55- 200917962 ch3ch2 # CH3(CH2)2 # (CH3)2CH,

R 53R 53

./N N I CHF../N N I CHF.

R N IR N I

2 A3.ef CHF2 A3.eg R N I chf2 A3.eh #2 A3.ef CHF2 A3.eg R N I chf2 A3.eh #

A3.ei A3.ekA3.ei A3.ek

A3.el A3.em A3.en A3.eo 。 適宜基團A3之其他實例係以下式之基團:A3.fa、 A3.fb、A3.fc、A3.fd、A3.fe、A3.ff、A3.fg、A3.fh、 A3.fi、A3.fk、A3.fl、A3.fm、A3.fn 及 A3.fo,其中 R53 係 如表A3之一列所定義(基團A3.fal-A3.fa81至A3.fol-A3.fo81):A3.el A3.em A3.en A3.eo. Further examples of suitable groups A3 are those of the formula: A3.fa, A3.fb, A3.fc, A3.fd, A3.fe, A3.ff, A3.fg, A3.fh, A3.fi, A3.fk, A3.fl, A3.fm, A3.fn and A3.fo, wherein R53 is as defined in one of the columns of Table A3 (group A3.fal-A3.fa81 to A3.fol-A3.fo81):

# η r.# η r.

# FHX# FHX

# F.HC# F.HC

# F,C# F,C

# A3.fa A3.fb A3.fc A3.fd CH3CH2 # CH3(CH2)2 # (CH3)2CHs ## A3.fa A3.fb A3.fc A3.fd CH3CH2 # CH3(CH2)2 # (CH3)2CHs #

r53^^ χΝ R N IR53^^ χΝ R N I

〇f3 A3.ff〇f3 A3.ff

A3.fl r53^^ R N Icf3 A3.fg # #A3.fl r53^^ R N Icf3 A3.fg # #

A3.fmA3.fm

R 5;R 5;

N I cf3 A3.fhN I cf3 A3.fh

A3.fi A3.fe # NC #A3.fi A3.fe # NC #

##

##

A3.fo 133661.doc -56- 200917962 除此之外,x3較佳係孤電子對。其中乂係〇之式域叫匕 合物亦稱為化合物I或II之N-氧化物。 除此之外,變量 Y、Ra、、RC、Rd、Re、Rf、Rg、 R、R及Ry較佳彼此獨立地具有以下含義之一: Y 係Ο ;A3.fo 133661.doc -56- 200917962 In addition, x3 is preferably a lone pair. The formula of the oxime system is also called the N-oxide of the compound I or II. In addition, the variables Y, Ra, RC, Rd, Re, Rf, Rg, R, R and Ry preferably have one of the following meanings independently of each other: Y system;

Ra、Rb、Re彼此獨立地選自氫、Ci_C4_烧基及Ci_C4_齒代 烧基; R係選自C〗_C4-烷基及CVC4-鹵代烷基; R、R彼此獨立地選自氫、Ci_C4_烷基,或 R及R與其所鍵結之氮原子—起形成5_或6員飽和雜環,其 可具有選自0、之另一雜原子作為環成員原子, 例如〇比嘻咬-1 _盖、丄与 疋丞/、風吡啶-1-基、嗎啉-4-基、六氫 °比嗪-1 -基或4-甲基六氫吡嗪_丨_基;Ra, Rb, and Re are each independently selected from the group consisting of hydrogen, Ci_C4_alkyl and Ci_C4_dentate; R is selected from C-C4-alkyl and CVC4-haloalkyl; R, R are independently selected from hydrogen, Ci_C4_alkyl, or R and R together with the nitrogen atom to which they are bonded form a 5- or 6-membered saturated heterocyclic ring, which may have another hetero atom selected from 0, as a ring member atom, such as a terpene bite -1 _ cap, hydrazine and hydrazine /, pyridin-1-yl, morpholin-4-yl, hexahydropyrazine-1-yl or 4-methylhexahydropyrazine 丨-yl;

Rg Rx R 'R1係彼此獨立地選自氫及Ci_C4_烷基;Rg Rx R 'R1 are independently selected from hydrogen and Ci_C4_alkyl;

Ry 係選自由以下組成之群:鹵素、氰基、硝基、Cl-C4-^基、CVC4-i代烧基、Ci_c4_烧氧基、c]心-鹵代烷 氧基、q-C4-烷基磺醯基及〇1&lt;4__代烷基磺醯基; 係選自Cl_C4_烷氧基、C3-C0-環烷基及苯基。 本3發明極佳實施例係關於式Hb合物及其鹽,其中χ1#〇 且X係孤電子對。在下文中該等化合物亦稱為化合物la。 0 广 a 人 (la) R1 R2 在式“中’變量^心尺^係如本文所定^在式 133661.doc -57- 200917962 “化&amp;物巾較佳者係彼等化合物,其中a係基團a卜例 如選自吡唑基Al.alA1.z81之基團。在式Ia化合物中較 佳者係彼等化合物,其中基團Rl、R2及R3中至少一個、較 佳基團R、R2及r3中至少兩個、且更佳所有基團r1、以 R3具有一種較佳含義。 尤佳貫施例係關於式la化合物及其鹽,其中 A係如本文所定義之基團A1,尤其為其中R4!、Rsi及r6i 具有較佳含義之基團A1,尤其為式A1 a至八丨z之吡唑 基’例如選自吡唑基A1,allA1 281之基團; R係氫、ci_c4-烷基或CVCV烷氧基-CVCV烷基,最佳 為氫、曱基或乙基; R2係選自氫、曱基、二氟甲基、三氟甲基、甲氧基、二 氟甲氧基及三氟曱氧基;且 R3係選自氫、甲基、二氟甲基、三氟甲基、甲氧基、二 氟甲氧基及三氟曱氧基;且較佳地其中基團…及尺3之 一個或兩個為氫。 此尤佳實施例之化合物之實例係下表丨至75中所列化合 物。 表1 :式1a化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團Al.al至Al.a81。 表2 : 式1a化合物及其鹽,其中R1係甲基,R2及R3為氣 且其中A係選自基團Al.a^A1.a8i。 表3 : 式1a化合物及其鹽,其中R1係乙基,r2&amp;r3為氫 且其中A係選自基團Ai.ai至Al.a81。 133661.doc -58- 200917962 表4 : 表5 : 表6 : 表7 : 表8 : 表9 : 表10 : 表11 : 表12 : 表13 : 表14 : 表15 : 式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團Al.bl至Al.b81。 式la化合物及其鹽,其中R〗係曱基,R2及R3為氫 且其中A係選自基團Al.bl至Al.b81。 式la化合物及其鹽,其中以係乙基,R2及R3為氫 且其中A係選自基團Al.bl至Al.b81。 式la化合物及其鹽,其中R!、尺2及R3係氫且其中A 係選自基團Al.cl至Al.c81。 式la化合物及其鹽,其中Ri係曱基,以及尺3為氫 且其中A係選自基團Al.cl至A1.C81。 式la化合物及其鹽,其中Ri係乙基,尺2及尺3為氣 且其中A係選自基團ai.ci至Ai.cgl。 式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中a 係選自基團Al.dl至Al.dSl。 式la化合物及其鹽’其中Ri係甲基,以及尺3為氫 且其中A係選自基團Al.dl至Al.d81。 式la化合物及其鹽,其中Ri係乙基,“及尺3為氫 且其中A係選自基團Al.dl至Al.d81。 式la化合物及其鹽,其中R〗、R2&amp;R3係氫且其中a 係選自基團Al.el至Al.e81。 式la化合物及其鹽,其中R〗係曱基,尺2及以為气 且其中A係選自基團Al.el至Al.e81。 式la化合物及其鹽,其中Ri係乙基,R2&amp;R3為氣 且其中A係選自基團Al.el至Al.e81。 133661.doc -59- 200917962 表16 :式h化合物及其鹽,其中Rl、尺2及尺3係氫且其中a 係選自基團A1. f 1至a 1. f 8 1。 表17 .式1a化合物及其鹽,其中R1係曱基,r2及R3為氫且 其中A係選自基團Al.fl至Al.fSl。 表18 :式1a化合物及其鹽,其中R1係乙基,R2&amp;R3為氫 且其中A係選自基團A1.f^A1.f81。 表19 :式&amp;化合物及其鹽,其中Ri、…及尺3係氫且其中a 係選自基團A1 .gl至A1 .g81。 表20 :式h化合物及其鹽,其中Ri係曱基,“及尺3為氫 且其中A係選自基團八1.§1至八1冶81。 表21 :式h化合物及其鹽,其中Ri係乙基,尺2及尺3為氫 且其中A係達自基團Ai.gi至Ai.ggi。 表22 :式1a化合物及其鹽,其中r〗、R2&amp;R3係氫且其中a 係選自基團A1 .hi至A1 .h8 1。 表23 :式la化合物及其鹽,其中Ri係曱基,“及尺3為氫 且其中A係選自基團Al.hl至Al.h81。 表24 :式la化合物及其鹽,其中Ri係乙基,尺2及尺3為氯 且其中A係選自基團Al.hl至Al.h81。 表25 :式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中a 係選自基團Al.il至Al.i81。 表26 :式la化合物及其鹽,其中R!係曱基,尺2及R3為氫 且其中A係選自基團Al.il至Al.i81。 表27 :式la化合物及其鹽,其中Ri係乙基,R2&amp;R3為氣 且其中A係選自基團Al.il至Al.i81。 133661.doc 60· 200917962 表28 :式h化合物及其鹽,其中Ri、“及尺3係氫且其中a 係選自基團Al.kl至Al.k81。 表29 :式la化合物及其鹽,其中Ri係曱基,…及尺3為氫 且其中A係選自基團Al.kl至Al.k81。 表30 :式la化合物及其鹽,其中Ri係乙基,尺2及尺3為氫 且其中A係選自基團Al.kl至Al.k81。 表31 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團Al.ll至A1.181。 表32 :式la化合物及其鹽,其中R〗係甲基,R2及R3為氫 且其中A係選自基團Al.ll至A1.181。 表33 :式la化合物及其鹽,其中尺]係乙基,R2及R3為氫 且其中A係選自基團A1.U至A1.181。 表34 :式la化合物及其鹽’其中r1、R2及R3係氫且其中A 係選自基團A1 .ml至A1 .m81。 表35 :式la化合物及其鹽,其中Ri係曱基,尺2及R3為氣 且其中A係選自基團Al.ml至Al.m81。 表36 :式la化合物及其鹽,其中R1係乙基,尺2及R3為氯 且其中A係選自基團Al.ml至Al.m81。 表37 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團Al.nl至Al.n81。 表38 :式la化合物及其鹽,其中R1係曱基,!^及R3為氮 且其中A係選自基團Al.nl至Al.n81。 表39 :式la化合物及其鹽,其中R1係乙基,R2及R3為氮 且其中A係選自基團Al.nl至Al.n81。 133661.doc -61 · 200917962 表40 :式la化合物及其鹽,其中R1、R2及r3係氫且其中A 係選自基團Al.ol至AI.08I。 表41 :式la化合物及其鹽,其中R1係曱基,尺2及R3為氫 且其中A係選自基團Al.ol至A1.081。 表42 :式la化合物及其鹽,其中R1係乙基,r2及R3為氯 且其中A係選自基團Al.ol至A1.081。 表43 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A1 .pi至A1 .p81。 表44 :式la化合物及其鹽,其中R1係曱基,R2及R3為氫 且其中A係選自基團Al.pl至Al.p81。 表45 :式la化合物及其鹽,其中R1係乙基,“及R3為氫 且其中A係選自基團Al.pl至Al.p81。 表46 :式la化合物及其鹽’其中Ri、:^及R3係氫且其中a 係選自基團Al.ql至Al.q81。 表47 :式1a化合物及其鹽,其中R1係甲基,汉2及R3為氫 且其中A係選自基團Al.ql至Al.q81。 ' 表48 :式1a化合物及其鹽,其中R1係乙基,r2&amp;r3為氫 且其中A係選自基團A1.q^A1 q81。 表49 :式la化合物及其鹽,其中R〗、R2&amp;R3係氫且其中a 係選自基團A1 .rl至A1 .r81。 表50 :式ia化合物及其鹽,其中Ri係曱基,…及R3為氫 且其中A係選自基團Al.rl至Al.r81。 表51 :式la化合物及其鹽,其中Ri係乙基,R2及R3為氫 且其中A係選自基團Al.rl至Al,r81。 133661.doc -62- 200917962 表52 :式la化合物及其鹽,其中Ri、尺2及R3係氫且其中a 係選自基團A1.s 1至A1 .s8 1。 表53 :式la化合物及其鹽,其中R〗係曱基,R2及R3為氫 且其中A係選自基團a1s1至ai.s81。 表54 :式la化合物及其鹽,其中Ri係乙基,R2及R3為氫 且其中A係選自基團ai.si至ai.s8i。 表55 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A1 .tl至A1 .t8 1。 表56 :式la化合物及其鹽,其中Ri係曱基,尺2及尺3為氫 且其中A係選自基團Al.tl至Al.t81。 表57 :式la化合物及其鹽,其中Ri係乙基,R2&amp;R3為氫 且其中A係選自基團Al.tl至Al.t81。 表58 :式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中A 係選自基團A1 · u 1至A1. u 8 1。 表59 :式la化合物及其鹽,其中係曱基,尺2及尺3為氳 且其中A係選自基團Al.ul至A1.U81。 表60 :式la化合物及其鹽,其中Ri係乙基,“及尺3為氫 且其中A係選自基團Al.ul至Al.u81。 表61 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團Al.vl至Al.v81。 表62 式ia化合物及其鹽,其中R1係曱基,R2及R3為氫 且其中A係選自基團Al.vl至Al.v81。 表63 :式la化合物及其鹽,其中Ri係乙基,R2&amp;R3為氫 且其中A係選自基團Al.vl至Al.v81。 133661.doc -63- 200917962 表64 : 表65 : 表66 : 表67 : 表68 : 表69 : 表70 : 表71 : 表72 : 表73 : 表74 : 表75 : 式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團Al.wl至A1.W81。 式la化合物及其鹽,其中R1係曱基,R2及R3為氮 且其中A係選自基團Al.wl至Al.w81。 式la化合物及其鹽,其中R1係乙基,R2及R3為氮 且其中A係選自基團Al.wl至Al.w81。 式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A1 .xl至A1 .x81。 式la化合物及其鹽,其中R1係曱基,尺2及R3為氮 且其中A係選自基團Al.xl至A1.X81。 式la化合物及其鹽,其中R1係乙基,&amp;2及R3為氯 且其中A係選自基團Al.xl至A1.X81。 式la化合物及其鹽,其中Ri、尺2及R3係氫且其中a 係選自基團A1 .yl至A1 .y81。 式la化合物及其鹽,其中Ri係甲基,R2&amp;R3為氣 且其中A係選自基團Al.yl至Al.y81。 式la化合物及其鹽,其中係乙基,尺2及尺3為氣 且其中A係選自基團Al.yl至Al.y81。 式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團Al.zl至Al.z81。 式1a化合物及其鹽,其中R1係甲基,R2及R3為氫 且其中A係選自基團αι·ζι至ai.z81。 式la化合物及其鹽,其中R!係乙基,…及尺3為氣 且其中A係選自基團Ai.zi至Ai.zgi。 133661.doc -64- 200917962 另一尤佳實施例係關於式13化合物及复睡, A係如本文所定義之基團-Γ其為、:中〜 及R62具有較佳含義之基團A2,尤其為式―至 A2.d〇之吼唾基,例如選自吼唑基wA2.aa81 至 A2.dol-A2.do81 之基團;Ry is selected from the group consisting of halogen, cyano, nitro, Cl-C4-^, CVC4-i alkyl, Ci_c4_alkoxy, c] heart-haloalkoxy, q-C4-alkane The sulfonyl group and the oxime 1 &lt; 4__alkylsulfonyl group; are selected from the group consisting of Cl_C4_alkoxy, C3-C0-cycloalkyl and phenyl. An excellent embodiment of the present invention relates to a compound of the formula Hb and a salt thereof, wherein χ1#〇 and X are orphaned electron pairs. These compounds are also referred to hereinafter as compound la. 0 广 a人(la) R1 R2 In the formula "中的变化^心尺^ is as defined in this article ^ in the formula 133661.doc -57- 200917962 "Chemical &amp; towel is preferred by their compounds, of which a The group a is, for example, a group selected from pyrazolyl Al.alA1.z81. Preferred among the compounds of formula Ia are those compounds wherein at least one of the groups R1, R2 and R3, at least two of the preferred groups R, R2 and r3, and more preferably all groups r1, have R3 A preferred meaning. A preferred embodiment is a compound of the formula la and a salt thereof, wherein A is a group A1 as defined herein, especially a group A1 wherein R4!, Rsi and r6i have the preferred meanings, especially the formula A1a to Barium z pyrazolyl 'for example, a group selected from pyrazolyl A1, allA1 281; R-hydrogen, ci_c4-alkyl or CVCV alkoxy-CVCV alkyl, most preferably hydrogen, decyl or ethyl R2 is selected from the group consisting of hydrogen, decyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy; and R3 is selected from hydrogen, methyl, difluoromethyl And trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy; and preferably wherein one or both of the group ... and the ruler 3 are hydrogen. Examples of the compounds of this preferred embodiment are the compounds listed in Tables 丨 to 75 below. Table 1 : Compounds of the formula 1a and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group consisting of the groups Al.al to Al.a81. Table 2: Compounds of the formula 1a and salts thereof, wherein R1 is methyl, R2 and R3 are gas and wherein A is selected from the group Al.a^A1.a8i. Table 3: Compounds of the formula 1a and salts thereof, wherein R1 is ethyl, r2&amp;r3 is hydrogen and wherein A is selected from the group Ai.ai to Al.a81. 133661.doc -58- 200917962 Table 4: Table 5: Table 6: Table 7: Table 8: Table 9: Table 10: Table 11: Table 12: Table 13: Table 14: Table 15: Compounds of formula la and their salts, Wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group consisting of the groups Al.bl to Al.b81. And a salt thereof, wherein R is a fluorenyl group, R2 and R3 are hydrogen and wherein A is selected from the group consisting of Al. bl to Al.b81. A compound of the formula la and a salt thereof, wherein the ethyl group, R2 and R3 are hydrogen and wherein A is selected from the group consisting of the groups Al.bl to Al.b81. A compound of the formula la and a salt thereof, wherein R!, 尺 2 and R3 are hydrogen and wherein A is selected from the group consisting of the groups Al.cl to Al.c81. And a salt thereof, wherein Ri is a fluorenyl group, and ampule 3 is hydrogen and wherein A is selected from the group consisting of the groups Al.cl to A1.C81. A compound of the formula la and a salt thereof, wherein Ri is an ethyl group, the rule 2 and the ruler 3 are a gas and wherein the A group is selected from the group ai.ci to Ai.cgl. A compound of the formula la and a salt thereof, wherein Ri, R2 &amp; R3 are hydrogen and wherein a is selected from the group consisting of the groups Al.dl to Al.dSl. A compound of the formula la and a salt thereof wherein Ri is a methyl group, and a ruthenium 3 is hydrogen and wherein A is selected from the group consisting of the groups Al.dl to Al.d81. a compound of the formula la and a salt thereof, wherein Ri is an ethyl group, "and the ruler 3 is hydrogen and wherein A is selected from the group consisting of the groups Al. dl to Al.d81. The compound of the formula la and its salt, wherein R, R2 & R3 are Hydrogen and wherein a is selected from the group consisting of the groups Al.el to Al.e81. The compound of the formula la and the salt thereof, wherein R is a fluorenyl group, the ruler 2 and the gas are selected and wherein the A group is selected from the group Al.el to Al. E81. A compound of the formula la and a salt thereof, wherein Ri is ethyl, R2 &amp; R3 is a gas and wherein A is selected from the group consisting of Al.el to Al.e81. 133661.doc -59- 200917962 Table 16: Compounds of formula h and a salt thereof, wherein R1, 尺2 and 尺3 are hydrogen and wherein a is selected from the group A1. f 1 to a 1. f 8 1. Table 17. Compounds of the formula 1a and salts thereof, wherein R1 is a fluorenyl group, r2 And R3 is hydrogen and wherein A is selected from the group consisting of the groups Al.fl to Al.fSl. Table 18: Compounds of the formula 1a and salts thereof, wherein R1 is ethyl, R2&amp; R3 is hydrogen and wherein A is selected from the group A1 .f^A1.f81. Table 19: Compounds of the formula &amp;amp; and their salts, wherein Ri, ... and 3 are hydrogen and wherein a is selected from the group A1.gl to A1.g81. Table 20: Compounds of formula h and a salt thereof, wherein Ri is a sulfhydryl group, "and the ruler 3 is hydrogen and wherein the A group is selected from the group VIII 1. § 1 to 八 1 s 81. Table 21: Compounds of the formula h and their salts, in which Ri is ethyl, the rule 2 and the rule 3 are hydrogen and wherein the A is from the group Ai.gi to Ai.ggi. Table 22: Compounds of the formula 1a and salts thereof, wherein r, R2 &amp; R3 are hydrogen and wherein a is selected from the group A1.hi to A1.h8. Table 23: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, "and the rule 3 is hydrogen and wherein A is selected from the group consisting of the groups Al.hl to Al.h81. Table 24: Compounds of the formula la and salts thereof, wherein Ri Is an ethyl group, the ruler 2 and the ruler 3 are chlorine and wherein the A group is selected from the group of Al.hl to Al.h81. Table 25: a compound of the formula la and a salt thereof, wherein Ri, R2 & R3 are hydrogen and wherein a is selected From the group Al.il to Al.i81. Table 26: Compounds of the formula la and salts thereof, wherein R! is a fluorenyl group, the sizing elements 2 and R3 are hydrogen and wherein the A group is selected from the group consisting of the groups Al.il to Al.i81. Table 27: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 &amp; R3 is a gas and wherein A is selected from the group consisting of the groups Al.il to Al.i81. 133661.doc 60· 200917962 Table 28: Compounds of the formula h and a salt thereof, wherein Ri, "and the ruler 3 are hydrogen and wherein a is selected from the group consisting of the groups Al.kl to Al.k81. Table 29: Compounds of the formula la and salts thereof, wherein the Ri-based fluorenyl group, and the calilem 3 are hydrogen and wherein the A group is selected from the group consisting of the groups Al.kl to Al.k81. Table 30: Compounds of the formula la and salts thereof, wherein Ri is ethyl, the rule 2 and the rule 3 are hydrogen and wherein A is selected from the group consisting of the groups Al.kl to Al.k81. Table 31: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group consisting of the groups Al.ll to A1.181. Table 32: Compounds of the formula la and salts thereof, wherein R is methyl, R2 and R3 are hydrogen and wherein A is selected from the group consisting of the groups Al.ll to A1.181. Table 33: Compounds of the formula la and salts thereof, wherein the ruthenium is an ethyl group, R2 and R3 are hydrogen and wherein the A group is selected from the group A1.U to A1.181. Table 34: Compounds of the formula la and salts thereof wherein r1, R2 and R3 are hydrogen and wherein A is selected from the group A1.ml to A1.m81. Table 35: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, the sizing elements 2 and R3 are a gas and wherein the A group is selected from the group consisting of the groups Al.ml to Al.m81. Table 36: Compounds of the formula la and salts thereof, wherein R1 is ethyl, the quaternary 2 and R3 are chloro and wherein A is selected from the group consisting of the groups Al.ml to Al.m81. Table 37: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group consisting of the groups Al.nl to Al.n81. Table 38: Compounds of the formula la and their salts, in which R1 is a fluorenyl group,! And R3 is nitrogen and wherein A is selected from the group consisting of the groups Al.nl to Al.n81. Table 39: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2 and R3 are nitrogen and wherein A is selected from the group consisting of the groups Al.nl to Al.n81. 133661.doc -61 · 200917962 Table 40: Compounds of the formula la and salts thereof, wherein R1, R2 and r3 are hydrogen and wherein A is selected from the group consisting of the groups Al.ol to AI.08I. Table 41: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, the sizing elements 2 and R3 are hydrogen and wherein the A group is selected from the group consisting of the groups Al.ol to A1.081. Table 42: Compounds of the formula la and salts thereof, wherein R1 is ethyl, r2 and R3 are chloro and wherein A is selected from the group consisting of the groups Al.ol to A1.081. Table 43: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A1.pi to A1.p81. Table 44: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, R2 and R3 are hydrogen and wherein A is selected from the group consisting of the groups Al.pl to Al.p81. Table 45: Compounds of the formula la and salts thereof, wherein R1 is ethyl, "and R3 is hydrogen and wherein A is selected from the group consisting of the groups Al.pl to Al.p81. Table 46: Compounds of the formula la and their salts" wherein Ri, And R3 are hydrogen and wherein a is selected from the group consisting of the groups Al.ql to Al.q81. Table 47: Compounds of the formula 1a and salts thereof, wherein R1 is methyl, Han 2 and R 3 are hydrogen and wherein A is selected from The group Al.ql to Al.q81. 'Table 48: A compound of the formula 1a and a salt thereof, wherein R1 is ethyl, r2&amp;r3 is hydrogen and wherein A is selected from the group A1.q^A1 q81. Table 49: And a salt thereof, wherein R, R2 and R3 are hydrogen and wherein a is selected from the group A1.rl to A1.r81. Table 50: Compounds of the formula ia and salts thereof, wherein Ri is a thiol group, ... R3 is hydrogen and wherein A is selected from the group consisting of the groups Al.rl to Al.r81. Table 51: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 and R3 are hydrogen and wherein A is selected from the group Al. Rl to Al, r 81. 133661.doc -62- 200917962 Table 52: Compounds of the formula la and salts thereof, wherein Ri, Ruler 2 and R3 are hydrogen and wherein a is selected from the group A1.s 1 to A1.s8 1 . Table 53: Compounds of the formula la and salts thereof, wherein R is a fluorenyl group, R2 and R3 are hydrogen and wherein A is selected from the group a1s1 to ai .s 81. Table 54: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 and R3 are hydrogen and wherein A is selected from the group ai.si to ai.s8i. Table 55: Compounds of the formula la and salts thereof, Wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A1.tl to A1.t8 1. Table 56: a compound of the formula la and a salt thereof, wherein the Ri is a sulfhydryl group, the ruler 2 and the ruler 3 are hydrogen and wherein A is selected from the group consisting of the groups Al.tl to Al.t81. Table 57: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group consisting of Al.tl to Al.t81 Table 58: Compounds of the formula la and salts thereof, wherein Ri, R2 &amp; R3 are hydrogen and wherein A is selected from the group A1 · u 1 to A1. u 8 1. Table 59: Compounds of the formula la and salts thereof, wherein曱 base, 尺 2 and 尺 3 are 氲 and wherein A is selected from the group consisting of Al.ul to A1.U81. Table 60: Compounds of formula la and salts thereof, wherein Ri is ethyl, "and ruler 3 is hydrogen and wherein A is selected from the group consisting of Al.ul to Al.u81. Table 61: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group consisting of the groups Al.vl to Al.v81. Table 62 Compounds of the formula ia and salts thereof, wherein R1 is a fluorenyl group, R2 and R3 are hydrogen and wherein A is selected from the group consisting of the groups Al.vl to Al.v81. Table 63: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group consisting of the groups Al.vl to Al.v81. 133661.doc -63- 200917962 Table 64: Table 65: Table 66: Table 67: Table 68: Table 69: Table 70: Table 71: Table 72: Table 73: Table 74: Table 75: Compounds of the formula la and their salts, Wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group consisting of the groups Al.wl to A1.W81. And a salt thereof, wherein R1 is a fluorenyl group, R2 and R3 are nitrogen and wherein A is selected from the group consisting of the groups Al.wl to Al.w81. And a salt thereof, wherein R1 is ethyl, R2 and R3 are nitrogen and wherein A is selected from the group consisting of Al.wl to Al.w81. A compound of the formula la and a salt thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A1.xl to A1.x81. A compound of the formula la and a salt thereof, wherein R1 is a fluorenyl group, the quaternary 2 and R3 are nitrogen and wherein the A group is selected from the group consisting of the groups Al.xl to A1.X81. And a salt thereof, wherein R1 is ethyl, &amp; 2 and R3 are chloro and wherein A is selected from the group consisting of the groups Al.xl to A1.X81. A compound of the formula la and a salt thereof, wherein Ri, the ruler 2 and the R3 are hydrogen and wherein a is selected from the group A1.yl to A1.y81. A compound of the formula la and a salt thereof, wherein Ri is a methyl group, R2 &amp; R3 is a gas and wherein A is selected from the group consisting of the groups Al.yl to Al.y81. A compound of the formula la and a salt thereof, wherein the ethyl group, the rule 2 and the ruler 3 are a gas and wherein the A group is selected from the group consisting of the groups Al.yl to Al.y81. A compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group consisting of the groups Al.zl to Al.z81. A compound of the formula 1a and a salt thereof, wherein R1 is methyl, R2 and R3 are hydrogen and wherein A is selected from the group αι·ζι to ai.z81. And a salt thereof, wherein R! is ethyl, and 3 is a gas and wherein A is selected from the group Ai.zi to Ai.zgi. 133661.doc -64- 200917962 Another preferred embodiment relates to a compound of formula 13 and a re-sleeping, group A as defined herein, which is a group A2 having the preferred meanings: In particular, the oxime group of the formula - to A2.d〇, for example, a group selected from the group consisting of carbazolyl groups wA2.aa81 to A2.dol-A2.do81;

R1 係氫、CVC4·烷基或CVCV烷氧基_ 佳為氫、曱基或乙基 ; R2 係選自氫、曱基、_ -鼠甲基、三 基、二氟甲氧基及三 氟甲氧基;且 R3 係選自氫、甲基、- 二氟甲基、三 基、二氟甲氧基及三 氟^曱乳基;J 氟甲基、甲氧 團R2及R3中一個或兩個為氫。 此 合物 尤佳實施例之化合物之實例係下表76至23丨中所列化 表76 :式h化合物及其鹽’其中Ri、R2&amp;R3係氫且其中a 係選自基團A2.aal至A2.aa8 1。 表77 ··式la化合物及其鹽,其中R1係甲基,R2及R3係氣 且其中A係選自基團A2.aal至A2.aa81。 表78 : 式la化合物及其鹽,其中R1係乙基,R2&amp;R3係氣 且其中A係選自基團A2.aal至A2.aa81。R1 is hydrogen, CVC4.alkyl or CVCV alkoxy is preferably hydrogen, fluorenyl or ethyl; R2 is selected from the group consisting of hydrogen, fluorenyl, _-murine methyl, tris, difluoromethoxy and trifluoro a methoxy group; and R3 is selected from the group consisting of hydrogen, methyl, -difluoromethyl, tris, difluoromethoxy, and trifluoromethane; one of J fluoromethyl, methoxyl R2, and R3 or Both are hydrogen. Examples of compounds of this preferred embodiment are the compounds listed in Tables 76 to 23 above: Formula h compounds and salts thereof wherein Ri, R2 & R3 are hydrogen and wherein a is selected from the group A2. Aal to A2.aa8 1. Table 77: A compound of the formula la and a salt thereof, wherein R1 is a methyl group, R2 and R3 are a gas, and wherein A is selected from the group A2.aal to A2.aa81. Table 78: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2&amp;R3 is a gas and wherein A is selected from the group A2.aal to A2.aa81.

表79 : 式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A2.abl至A2.ab81。 表80 : 式la化合物及其鹽,其中R1係曱基,R2及R3係氣 且其中A係選自基團A2.abl至A2.ab81。 133661.doc -65- 200917962 表81 :式la化合物及其鹽,其中Ri係乙基,以及尺3係氣 且其中A係選自基團A2.abl至A2.ab81。 表82 :式la化合物及其鹽,其中r1、R2及R3係氫且其中a 係選自基團A2.acl至A2.ac81。 表83 :式la化合物及其鹽,其中R1係甲基,R2&amp;R3係氫 且其中A係選自基團A2.acl至A2.ac81。 表84 :式la化合物及其鹽,其中R1係乙基,R2&amp;R3係氣 且其中A係選自基團A2.acl至A2.ac81。 表85 :式la化合物及其鹽,其中r1、R2及R3係氫且其中A 係選自基團A2,adl至A2.ad81。 表86 :式la化合物及其鹽,其中R1係甲基,以及尺3係氣 且其中A係選自基團A2.adl至A2.ad81。 表87 :式la化合物及其鹽,其中R1係乙基,1^2及R3係氣 且其中A係選自基團A2.adl至A2.ad81。 表88 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A2.ael至A2.ae81。 表89 :式la化合物及其鹽,其中R1係甲基,R2及R3係氣 且其中A係選自基團A2.ael至A2.ae81。 表90 : 式la化合物及其鹽,其中R1係乙基,R2及R3係氣 且其中A係選自基團A2.ael至A2.ae81。 表91 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A2.afl至A2.af81。 表92 :式la化合物及其鹽,其中R1係甲基,R2及R3係氣 且其中A係選自基團A2.afl至A2.af81。 I33661.doc -66- 200917962 表93 :式la化合物及其鹽,其中W係乙基,尺2及R3係氣 且其中A係選自基團A2.afl至A2.af81。 表94 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A2.agl至A2.ag81。 表95 :式la化合物及其鹽,其中R1係甲基,R2及R3係氣 且其中A係選自基團A2.agl至A2.ag81。 表96 :式la化合物及其鹽,其中R1係乙基,以及尺3係氣 且其中A係選自基團A2.ahl至A2.ah81。 表97 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A2.ail至A2.ai81。 表98 :式la化合物及其鹽,其中R1係甲基,以及尺3係氣 且其中A係選自基團A2.ail至A2.ai81。 表99 :式la化合物及其鹽,其中R1係乙基,R2&amp;R3係氣 且其中A係遠自基團A2.ail至A2.ai81。 表100 :式la化合物及其鹽,其中R1、R2&amp;R3係氫且其中A 係選自基團A2.akl至A2.ak81。 表101 :式la化合物及其鹽,其中R〗係曱基,…及尺3係氫 且其中A係選自基團A2.akl至A2.ak81。 表102 :式la化合物及其鹽,其中Rl係乙基,R2&amp;R3係氫 且其中A係選自基團A2.akl至A2.ak81。 表103 :式la化合物及其鹽,其中Ri、…及尺3係氫且其中A 係選自基團A2.all至A2.al81。 表104 :式la化合物及其鹽,其中…係甲基,R2及R3係氫 且其中A係選自基團A2.all至A2.al81。 133661.doc -67- 200917962 表105 :式la化合物及其鹽,其中R1係乙基,尺2及R3係氫 且其中A係選自基團A2.all至A2.al81。 表106 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A2.aml至A2.am81。 表107 :式la化合物及其鹽,其中R1係甲基,r2及R3係氣 且其中A係選自基團A2.aml至A2.am81。 表1 08 :式la化合物及其鹽,其中R1係乙基,R2及R3係氣 且其中A係選自基團A2.aml至A2.am81。 表109 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A2.anl至A2.an81 〇 表110 :式la化合物及其鹽,其中R1係甲基,R2及R3係氫 且其中A係選自基團A2.anl至A2.an81。 表Π 1 :式la化合物及其鹽,其中R1係乙基,R2及r3係氣 且其中A係選自基團A2.anl至A2.an81 〇 表112 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A2.aol至A2.ao81。 表11 3 :式la化合物及其鹽,其中R1係甲基,R2及R3係氫 且其中A係選自基團A2.aol至A2.ao81。 表114 :式la化合物及其鹽,其中R1係乙基,尺2及R3係氣 且其中A係選自基團A2.aol至A2.ao81。 表U 5 :式la化合物及其鹽,其中r1、R2及R3係氫且其中a 係選自基團A2.bal至A2.ba81。 表116 :式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氣 且其中A係選自基團A2.bal至A2.ba81。 133661.doc -68- 200917962 表1 17 :式la化合物及其鹽,其中Ri係乙基,尺2及R3係氫 且其中A係選自基團A2.bal至A2.ba81。 表118 :式la化合物及其鹽,其中r1 '尺2及R3係氫且其中A 係選自基團A2.bbl至A2.bb81。 表119 :式la化合物及其鹽,其中Ri係甲基,R2及R3係氫 且其中A係選自基團A2.bbl至A2.bb81。 表120 :式la化合物及其鹽,其中r1係乙基,R2及R3係氫 且其中A係選自基團A2.bbl至A2.bb81。 表121 :式la化合物及其鹽,其中ri、尺2及R3係氫且其中a 係選自基團A2.bcl至A2.bc81。 表122 :式la化合物及其鹽,其中Ri係甲基,尺2及R3係氫 且其中A係選自基團A2.bcl至A2.bc81。 表123 :式la化合物及其鹽,其中Ri係乙基,尺2及R3係氫 且其中A係選自基團A2.bcl至A2.bc81。 表124 :式la化合物及其鹽,其中ri、R2及R3係氫且其中A 係選自基團A2.bdl至A2.bd81。 表125 :式la化合物及其鹽,其中r1係甲基,r2及R3係氮 且其中A係選自基團A2.bdl至A2.bd81。 表126 :式la化合物及其鹽,其中Ri係乙基,R2及R3係氫 且其中A係選自基團A2.bdl至A2.bd81。 表127 :式la化合物及其鹽,其中r'·、R2及R3係氫且其中A 係選自基團A2.bel至A2.be81。 表128 :式la化合物及其鹽,其中R1係曱基,R2及R3係氫 且其中A係選自基團A2.bel至A2.be81。 133661.doc -69- 200917962 表129 :式la化合物及其鹽,其中Ri係乙基,R2&amp;R3係氫 且其中A係選自基團A2.bel至A2.be81。 表130 :式la化合物及其鹽,其中Ri、尺2及尺3係氫且其中a 係選自基團A2.bfl至A2.bf81。 表131 :式la化合物及其鹽,其中R〗係甲基,尺2及R3係氫 且其中A係選自基團A2.bfl至A2.bf81。 表132 :式la化合物及其鹽,其中Ri係乙基,尺2及R3係氫 且其中A係選自基團A2.bfl至A2.bf81。 表133 :式la化合物及其鹽,其中Ri、…及尺3係氫且其中A 係選自基團A2.bgl至A2.bg81。 表134 :式la化合物及其鹽,其中Ri係曱基,尺2及R3係氫 且其中A係選自基團A2.bgi至A2.bg81。 表135 :式la化合物及其鹽,其中Ri係乙基,尺2及尺3係氫 且其中A係選自基團A2.bhl至A2.bh8 1。 表136 :式la化合物及其鹽,其中Ri、尺2及尺3係氫且其中A 係選自基團A2.bil至A2.bi81。 表137 :式la化合物及其鹽,其中係曱基,R2&amp;R3係氫 且其中A係選自基團A2.bil至A2.bi81。 表138 :式la化合物及其鹽,其中Ri係乙基,R2及R3係氫 且其中A係選自基團A2.bil至A2.bi81。 表139 :式la化合物及其鹽,其中R〗、R2&amp;R3係氫且其中a 係選自基團A2.bkl至A2.bk81。 表140 :式la化合物及其鹽,其中Ri係甲基,以及尺3係氫 且其中A係選自基團A2.bkl至A2.bk81。 133661 .doc -70- 200917962 表14 1 :式la化合物及其鹽,其中R1係乙基,R2及r3係氣 且其中A係選自基團A2.bkl至A2.bk81。 表142 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A2.bll至A2.bl81。 表143 :式la化合物及其鹽,其中R1係甲基,以及尺3係氣 且其中A係選自基團A2.bll至A2.M81。 表144 :式la化合物及其鹽,其中係乙基,R2&amp;R3係氣 且其中A係選自基團A2.M1至A2.bl81。 表145 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A2.bml至A2.bm81。 表146 :式la化合物及其鹽,其中R1係曱基,R2及R3係氣 且其中A係選自基團A2.bml至A2,bm81。 表147 :式la化合物及其鹽,其中R1係乙基,r2及R3係氣 且其中A係選自基團A2.bml至A2.bm81。 表148 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A2,bnl至A2.bn81。 表149 :式la化合物及其鹽,其中R1係曱基,R2及R3係氯 且其中A係選自基團A2.bnl至A2.bn81。 表150 :式la化合物及其鹽,其中r〗係乙基,R2&amp;R3係氣 且其中A係選自基團A2.bnl至A2.bn81。 表151 :式la化合物及其鹽,其中r】、r2&amp;r3係氫且其中A 係選自基團A2.bol至A2.bo81。 表152 :式la化合物及其鹽,其中R1係甲基,R2及R3係氣 且其中A係選自基團A2.bol至A2.bo81。 133661.doc 200917962 表 153 : 表 154 : 表 155 : 表 156 : 表 157 : 表 158 : 表 159 : 表 160 : 表 161 : 表 162 : 表 163 : 表 164 : 式la化合物及其鹽,其中係乙基,R2及R3係氣 且其中A係選自基團A2.bol至A2.bo81。 式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A2.cal至A2.ca81。 式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氣 且其中A係選自基團A2.cal至A2.ca81。 式la化合物及其鹽,其中Ri係乙基,以及汉3係氣 且其中A係選自基團A2.cal至A2.ca81。 式la化合物及其鹽,其中Ri、…及尺3係氫且其中a 係選自基團A2.cbl至A2.cb81。 式la化合物及其鹽,其中Ri係曱基,以及尺3係氫 且其中A係通自基團A2.cb 1至A2.cb8 1。 式la化合物及其鹽,其中Ri係乙基,以及尺3係氣 且其中A係選自基團A2.cbl至A2.cb81。 式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A2.ccl至A2.cc81。 式la化合物及其鹽,其中Ri係曱基,R2&amp;R3係氫 且其中A係選自基團A2.cc 1至A2.cc81。 式la化合物及其鹽,其中R〗係乙基,R2&amp;R3係氫 且其中A係選自基團A2.ccl至A2.cc81。 式1a化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A2.cdl至A2.cd81。 式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氣 且其中A係選自基團A2.cdl至A2.cd81。 133661.doc -72- 200917962 表165 :式la化合物及其鹽,其中Ri係乙基,尺2及尺3係氫 且其中A係選自基團A2.cdl至A2.cd81。 表166 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A2.cel至A2.ce81。 表167 :式la化合物及其鹽,其中Ri係甲基,尺2及R3係氫 且其中A係選自基團A2.cel至A2.ce81。 表168 :式la化合物及其鹽,其中Ri係乙基,“及尺3係氯 且其中A係選自基團A2.cel至A2.ce81。 表169 :式la化合物及其鹽,其中Ri、…及尺3係氫且其中A 係選自基團A2.cfl至A2.cf81。 表170 :式la化合物及其鹽,其中Ri係甲基,…及尺3係氫 且其中A係選自基團A2.cfl至A2.cf81。 表171 :式la化合物及其鹽,其中Ri係乙基,…及汉3係氣 且其中A係選自基團A2.cfl至A2.cf81。 表172 :式la化合物及其鹽,其中Ri、尺2及尺3係氫且其中a 係選自基團A2.cgl至A2.cg81。 表173 :式la化合物及其鹽,其中Ri係曱基,尺2及汉3係氮 且其中A係選自基團A2.cgl至A2.cg81。 表174 :式la化合物及其鹽,其中Ri係乙基,尺2及R3係氯 且其中A係選自基團A2.chl至A2.ch81。 表175 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A2,cil至A2.ci81。 表176 :式la化合物及其鹽,其中Ri係甲基,尺2及R3係氮 且其中A係選自基團A2.cil至A2.ci81。 133661.doc -73- 200917962 表177 :式la化合物及其鹽,其中Ri係乙基,尺2及R3係氫 且其中A係選自基團A2.cil至A2.ci81。 表178 :式la化合物及其鹽,其中r1、R2及R3係氫且其中a 係選自基團A2.ckl至A2.ck81。 表179 :式la化合物及其鹽,其中R1係甲基,R2&amp;R3係氫 且其中A係選自基團A2.ckl至A2.ck81。 表180 :式la化合物及其鹽,其中R1係乙基,尺2及R3係氣 且其中A係選自基團A2.ckl至A2.ck81。 表181 :式la化合物及其鹽,其中r1、R2及R3係氫且其中A 係選自基團A2.cll至A2.cl81。 表182 :式la化合物及其鹽’其中R!係曱基,尺2及R3係氯 且其中A係選自基團A2.cll至A2.C181。 表183 :式la化合物及其鹽,其中R1係乙基,R2&amp;R3係氣 且其中A係選自基團A2.cll至A2.C181。 表184 :式la化合物及其鹽’其中Ri、R2及R3係氫且其中a 係選自基團A2.cml至A2.cm81。 表185 :式la化合物及其鹽,其中Ri係曱基,R2及R3係氣 且其中A係選自基團A2.cml至A2.cm81。 表186 :式la化合物及其鹽,其中R1係乙基,R2及R3係氣 且其中A係選自基團A2.cml至A2.cm81。 表187 :式la化合物及其鹽,其中r1、R2及R3係氫且其中a 係選自基團A2.cnl至A2.en81。 表1 8 8 :式la化合物及其鹽,其中Ri係甲基,R2及R3係氣 且其中A係選自基團A2.cnl至A2.cn81。 133661.doc •74- 200917962 表189 :式la化合物及其鹽’其中r1係乙基,汉2及R3係氣 且其中A係選自基團A2.cnl至A2.cn81。 表190 :式la化合物及其鹽,其中r〗、r2及R3係氫且其中a 係選自基團A2.col至A2.co81。 表191 :式la化合物及其鹽,其中Ri係曱基,R2&amp;R3係氣 且其中A係選自基團A2.col至A2.co81。 表192 :式la化合物及其鹽,其中Ri係乙基,以及尺3係氣 且其中A係選自基團A2.co 1至A2.co8 1。 表193 :式la化合物及其鹽,其中Ri、尺2及R3係氫且其中a 係選自基團A2.dal至A2.da81。 表194 :式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氫 且其中A係選自基團A2.dal至A2.da81。 表195 :式la化合物及其鹽,其中R】係乙基,R2&amp;R3係氣 且其中A係選自基團A2.dal至A2.da81。 表196 :式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中A 係選自基團A2.dbl至A2.db81。 表197 :式la化合物及其鹽,其中Ri係曱基,R2及R3係氫 且其中A係選自基團A2.dbl至A2.db81。 表198 :式la化合物及其鹽,其中Ri係乙基,R2&amp;R3係氫 且其中A係選自基團A2此丨至A2.db81。 表199 :式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中A 係選自基團A2.dcl至A2.dc81。 表200 :式la化合物及其鹽,其中Ri係甲基,尺2及R3係氫 且其中A係選自基團A2.dcl至A2.dc81。 133661.doc -75- 200917962 表 201 : 表 202 : 表 203 : 表 204 : 表 205 : 表 206 : 表 207 : 表 208 : 表 209 ·· 表 210 : 表 211 : 表 212 : 式la化合物及其鹽’其中R1係乙基,尺2及R3係氯 且其中A係選自基團A2.dcl至A2.dc81。 式la化合物及其鹽’其中R〗、R2及R3係氫且其中A 係選自基團A2.ddl至A2.dd81。 式la化合物及其鹽,其中R〗係甲基,以及尺3係氨 且其中A係選自基團A2.ddl至A2.dd81。 式la化合物及其鹽,其中r〗係乙基,R2&amp;R3係氣 且其中A係選自基團A2.ddl至A2.dd81。 式la化合物及其鹽,其中r1、R2及R3係氫且其中A 係選自基團A2.del至A2.de81。 式la化合物及其鹽,其中係甲基,…及尺3係氫 且其中A係選自基團A2.del至A2.de81。 式la化合物及其鹽,其中Ri係乙基,…及尺3係氯 且其中A係選自基團A2.del至A2.de81。 式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中A 係選自基團A2.dfl至A2.df81。 式la化合物及其鹽,其中Ri係曱基,尺2及尺3係氫 且其中A係選自基團A2.dfl至A2.df81。 式la化合物及其鹽,其中Ri係乙基,R2&amp;R3係氫 且其中A係選自基團A2.dfl至A2.df81。 式la化合物及其鹽,其中、R2及R3係氫且其中A 係選自基團A2.dgl至A2.dg81。 式1a化合物及其鹽,其中R〗係曱基,R2及R3係氫 且其中A係選自基團A2.dgl至A2.dg81。 133661.doc -76- 200917962 表213 :式la化合物及其鹽,其中R]係乙基,R2&amp;R3係氣 且其中A係選自基團A2.dhl至A2.dh81。 表214 :式la化合物及其鹽,其中Ri、R2&amp;R3係氣且其中a 係選自基團A2.dil至A2.di81。 表215 :式la化合物及其鹽,其中Ri係甲基’ R2&amp;R3係氫 且其中A係選自基團A2.dil至A2.di81。 表216 :式la化合物及其鹽,其中Ri係乙基,以及尺3係氣 且其中A係選自基團A2.dil至A2.di81。 表217 :式1a化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A2.dkl至A2.dk81。 表218 :式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氫 且其中A係選自基團A2.dkl至A2.dk81。 表219 :式la化合物及其鹽,其中Ri係乙基,以及尺3係氣 且其中A係選自基團A2.dkl至A2.dk81。 表220 :式la化合物及其鹽,其中Ri、尺2及尺3係氫且其中a 係選自基團A2.dll至A2.dl81。 、 表221:式13化合物及其鹽,其中111係甲基,112及113係氫 且其中A係選自基團A2.dll至A2.dl81。 表222 :式la化合物及其鹽,其中Ri係乙基,以及汉3係氫 且其中A係選自基團A2.dll至A2.dl81。 表223 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A2.dml至A2.dm81。 表224 :式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氫 且其中A係選自基團A2.dml至A2.dm81。 133661.doc -77- 200917962 表225 表226 表227 表228 (' 表 229 表230 表231 另一 A \ R1 R2 R3 :式la化合物及其鹽,其中Ri係乙基,R2&amp;R3係氫 且其中A係選自基團A2.dml至A2.dm81。 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A2.dnl至A2.dn81。 :式la化合物及其鹽,其中Ri係甲基,…及尺3係氫 且其中A係選自基團八2(1111至八2.(11181。 :式la化合物及其鹽,其中Ri係乙基,R2&amp;R3係氫 且其中A係選自基團A2.dnl至A2.dn81。 :式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中a 係選自基團A2.dol至A2.do81。 :式la化合物及其鹽,其中Ri係曱基,“及尺3係氫 且其中A係選自基團A2.dol至A2.do81。 :式la化合物及其鹽,其中Ri係乙基,R2及R3係氫 且其中A係選自基團A2.dol至A2,do81。 尤佳實施例係關於式la化合物及其鹽,其中 係如本文所定義之基團A3 ’尤其為其中r43、r53 及R63具有較佳含義之基團A3 ,尤其為式八3⑽至 A3.do之吡唑基,例如選自吡唑基A3 aal_A3旳81 至 A3.dol-A3.do81 之基團; 係氫、C丨-CV烷基或Cl_C4_烷氧基·CpC2·烷基,最 佳為氫、甲基或乙基; 係選自氫、甲基、二氟甲基、三氟甲基、曱氧 基、二氣曱氧基及三氟曱氧基;且 係選自氫、甲基、二氟甲基、三氟曱基、甲氧 133661.doc -78- 200917962 基、二氟甲氧基及三氟甲氧基;且其中基團…及 R3中一個或兩個為氫。 此尤佳實施例之化合物之實例係下表2;32至477中所列化 合物。 表232 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A3.aal至A3.aa81。 表233 :式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氫 且其中A係選自基團A3.aal至A3.aa81。 表234 :式la化合物及其鹽,其中R〗係乙基,R2及R3係氫 且其中A係選自基團A3.aal至A3.aa81。 表235 :式la化合物及其鹽,其中R!、R2及R3係氫且其中a 係選自基團A3.abl至A3.ab81。 表236 :式la化合物及其鹽,其中Ri係曱基,…及尺3係氫 且其中A係選自基團A3,abl至A3.ab81。 表237 :式la化合物及其鹽,其中Ri係乙基,…及尺3係氫 且其中A係選自基團A3.abl至A3.ab81。 表238 :式la化合物及其鹽,其中、R2及R3係氫且其中a 係選自基團A3.acl至A3.ac81。 表239 :式la化合物及其鹽,其中Ri係甲基,以及尺3係氫 且其中A係選自基團A3.acl至A3.ac81。 表240 :式la化合物及其鹽,其中Ri係乙基,R2及R3係氫 且其中A係選自基團A3.acl至A3.ac81。 表241 :式la化合物及其鹽,其中Ri、以及尺3係氫且其中a 係選自基團A3,adl至A3.ad81。 133661.doc •79- 200917962 表242 :式la化合物及其鹽,其中Ri係甲基,汉2及R3係氫 且其中A係選自基團A3.adl至A3.ad81。 表243 :式la化合物及其鹽,其中Ri係乙基,R2及R3係氯 且其中A係選自基團A3.adl至A3.ad81。 表244 :式la化合物及其鹽,其中ri、R2及R3係氫且其中a 係選自基團A3.ael至A3.ae8 1。 表245 :式la化合物及其鹽,其中Ri係甲基,…及R3係氫 且其中A係選自基團A3.ael至A3.ae81。 表246 :式la化合物及其鹽,其中Ri係乙基,尺2及尺3係氫 且其中A係選自基團A3.ael至A3.ae81。 表247 :式la化合物及其鹽,其中ri、R2及R3係氫且其中a 係選自基團A3.afl至A3.af81。 表248 :式la化合物及其鹽,其中Ri係甲基,…及汉3係氫 且其中A係選自基團A3.ai l至A3.af81。 表249 :式la化合物及其鹽,其中Ri係乙基,尺2及汉3係氫 且其中A係選自基團A3.afl至A3.af81。 表250 :式la化合物及其鹽,其中Ri、尺2及尺3係氫且其中a 係選自基團A3.agl至A3.ag81。 表251 :式la化合物及其鹽,其中Ri係曱基,…及汉3係氫 且其中A係遥自基團A3.agl至A3.ag81。 表252 :式la化合物及其鹽,其中Rl係乙基,…及汉3係氫 且其中A係選自基團A3.agl至A3.ag81。 表253 :式la化合物及其鹽,其中Ri、尺2及尺3係氫且其中a 係選自基團A3.ahl至A3.ah81。 133661.doc -80- 200917962 表 254 : 表 255 : 表 256 : 表 257 : 表 258 : 表 259 : 表 260 : 表 261 : 表 262 : 表 263 : 表 264 : 表 265 : 式la化合物及其鹽,其中Rl係甲基,R2及R3係氫 且其中A係選自基團A3.ahl至A3.ah81。 式la化合物及其鹽,其中係乙基,R2及R3係氫 且其中A係選自基團A3.ahl至A3.ah81。 式1a化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團八3.&amp;丨1至八3义81。 式la化合物及其鹽,其中Ri係曱基,尺2及汉3係氣 且其中A係遥自基團A3.ail至A3.ai81。 式la化合物及其鹽,其中R]係乙基,R2及R3係氣 且其中A係選自基團A3,ail至A3.ai81。 式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A3.akl至A3.ak81。 式la化合物及其鹽,其中Ri係甲基,尺2及尺3係氫 且其中A係選自基團A3.akl至A3.ak81。 式la化合物及其鹽,其中Ri係乙基,以及尺3係氫 且其中A係選自基團A3.akl至A3.ak81。 式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A3.all至A3.al81。 式la化合物及其鹽,其中Ri係曱基,尺2及R3係氫 且其中A係選自基團A3.all至A3.al81。 式la化合物及其鹽’其中R〗係乙基,汉2及R3係氫 且其中A係選自基團A3.all至A3.al81。 式la化合物及其鹽,其中R1、尺2及R3係氫且其中A 係選自基團八3.壮1111至八3.311181。 I33661.doc -81 - 200917962 表 266 : 表 267 : 表 268 : 表 269 : 表 270 : 表 271 : 表 272 : 表,273 : 表 274 : 表 275 : 表 276 : 表 277 : 式la化合物及其鹽,其中Rl係甲基,以及汉3係氣 且其中A係選自基團A3.aml至A3.am81。 式la化合物及其鹽’其中以係乙基,以及汉3係氣 且其中A係選自基團A3 .am 1至A3 ,am8 1。 式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.anl至A3.an81。 式la化合物及其鹽,其中Rl係曱基,以及尺3係氣 且其中A係選自基團A3.anl至A3.an81。 式la化合物及其鹽’其中Ri係乙基,尺2及R3係氣 且其中A係選自基團A3.anl至A3.an81。 式la化合物及其鹽,其中R〗、…及尺3係氫且其中a 係選自基團A3.aol至A3.ao81。 式la化合物及其鹽,其中…係甲基,尺2及汉3係氫 且其中A係遥自基團A^.aol至A3.ao81。 式la化合物及其鹽,其中R〗、“及R3係氫且其中a 係選自基團A3.bal至A3.ba81。 式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氫 且其中A係選自基團A3.bal至A3.ba81。 式la化合物及其鹽’其中Ri係乙基,R2及R3係氫 且其中A係選自基團A3.bal至A3.ba81。 式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A3.bbl至A3.bb81。 式la化合物及其鹽,其中Ri係甲基,以及尺3係氫 且其中A係選自基團A3.bbl至A3.bb81。 133661.doc -82- 200917962 表 278 : 表 279 : 表 280 : 表 281 : 表 282 : 表 283 : 表 284 : 表 285 : 表 286 : 表 287 : 表 288 : 表 289 : 式la化合物及其鹽,其中Ri係乙基,以及尺3係氣 且其中A係選自基團A3.bbl至A3.bb81。 式la化合物及其鹽,其中r1、r2及R3係氫且其中A 係選自基團A3.bcl至A3.bc81。 式la化合物及其鹽,其中Ri係甲基,以及尺3係氣 且其中A係選自基團A3.bcl至A3.bc81。 式la化合物及其鹽,其中係乙基,以及汉3係氣 且其中A係選自基團A3.bci至A3.bc81。 式la化合物及其鹽’其中Ri、R2及R3係氫且其中a 係選自基團A3.bdl至A3.bd81。 式la化合物及其鹽,其中Ri係甲基,R2及R3係氣 且其中A係選自基團A3.bdl至A3.bd81。 式la化合物及其鹽,其中係乙基,R2&amp;R3係氣 且其中A係選自基團A3.bdl至A3.bd81。 式la化合物及其鹽,其中Ri、以及尺3係氫且其中a 係選自基團A3.bel至A3.be81。 式la化合物及其鹽,其中Ri係曱基,R2及R3係氣 且其中A係選自基團A3.bel至A3.be81。 式la化合物及其鹽,其中Ri係乙基,R2及R3係氣 且其中A係選自基團A3.bel至A3.be81。 式la化合物及其鹽,其中R〗、尺2及R3係氫且其中a 係選自基團A3.bfl至A3.bf81。 式1a化合物及其鹽’其中R1係甲基,R2及R3係氣 且其中A係選自基團A3.bfl至A3.bf81。 133661.doc -83- 200917962 表290 :式la化合物及其鹽,其中Ri係乙基,尺2及R3係氫 且其中A係選自基團A3.bfl至A3.bf81。 表291 :式la化合物及其鹽,其中r1、R2及R3係氫且其中A 係選自基團A3.bgl至A3.bg81。 表292 :式la化合物及其鹽,其中R〗係甲基,以及R3係氣 且其中A係選自基團A3.bgl至A3.bg81。 表293 :式la化合物及其鹽,其中Ri係乙基,R2&amp;R3係氣 且其中A係選自基團A3.bgl至A3.bg81。 表294 :式la化合物及其鹽,其中R1、尺2及尺3係氫且其中A 係選自基團A3.bhl至A3.bh81。 表295 :式la化合物及其鹽,其中R1係曱基,尺2及R3係氯 且其中A係選自基團A3.bhl至A3.bh81。 表296 :式la化合物及其鹽,其中R1係乙基,R2及R3係氣 且其中A係選自基團A3.bhl至A3.bh81。 表297 :式la化合物及其鹽,其中r1、R2及R3係氫且其中A 係選自基團A3.bil至A3.bi81。 表298 :式la化合物及其鹽,其中R1係曱基,尺2及R3係氣 且其中A係選自基團A3.bil至A3.bi81。 表299 :式la化合物及其鹽,其中R1係乙基,r2及R3係氣 且其中A係選自基團A3.bil至A3.M81。 表300 :式la化合物及其鹽,其中R1·、R2及r3係氫且其中A 係選自基團A3.bkl至A3.bk81。 表3 0 1 :式la化合物及其鹽,其中R1係甲基,r2及R3係氣 且其中A係選自基團A3.bkl至A3.bk81。 133661.doc -84 - 200917962 表302 :式la化合物及其鹽,其中Rl係乙基,…及汉3係氫 且其中A係選自基團A3.bkl至A3.bk81。 表303 .式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.bll至A3.bl81。 表304 :式la化合物及其鹽,其中…係甲基,R2及R3係氫 且其中A係選自基團A3.M1至A3.bl81。 表305 :式la化合物及其鹽,其中Ri係乙基,…及尺3係氫 且其中A係選自基團A3.M1至A3.bl81。 表306 :式la化合物及其鹽,其中、尺2及尺3係氫且其中a 係選自基團A3.bml至A3.bm81。 表307 :式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氫 且其中A係選自基團A3.bml至A3.bm81。 表308 :式la化合物及其鹽,其中N係乙基,“及尺3係氫 且其中A係選自基團A3.bml至A3.bm81。 表309 :式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中a 係選自基團A3.bnl至A3.bn81。 表310 :式la化合物及其鹽,其中Ri係曱基,R2及R3係氫 且其中A係選自基團A3 bnl至A3,bn81。 表311 :式la化合物及其鹽,其中Ri係乙基,…及尺3係氫 且其中A係選自基團A3.bnl至A3.bn81。 表312 :式la化合物及其鹽’其中Ri、R2及R3係氫且其中a 係選自基團A3.bol至A3.bo81。 表3 1 3 :式la化合物及其鹽,其中係甲基,R2及R3係氣 且其中A係選自基團A3.bol至A3.bo81。 133661.doc * 85 - 200917962 表314 :式la化合物及其鹽,其中R〗、以及尺3係氫且其中A 係選自基團A3.cal至A3.ca81。 表315 :式la化合物及其鹽,其中R1係甲基,以及尺3係氣 且其中A係選自基團A3.cal至A3.ca81。 表316 :式la化合物及其鹽,其中R1係乙基,R2&amp;R3係氣 且其中A係選自基團A3.cal至A3.ca81。 表317 :式la化合物及其鹽,其中r1、R2及R3係氫且其中A 係選自基團A3.cbl至A3.cb81。 表318 :式la化合物及其鹽,其中R1係曱基,以及R3係氣 且其中A係選自基團A3.cbl至A3.cb81。 表319 :式la化合物及其鹽,其中R1係乙基,尺2及R3係氣 且其中A係選自基團A3.cbl至A3.cb81。 表320 :式la化合物及其鹽,其中r1、R2及R3係氫且其中A 係選自基團A3.ccl至A3.cc81。 表321 :式la化合物及其鹽,其中Ri係甲基,R2及R3係氣 且其中A係選自基團A3.ccl至A3.cc81。 表322 :式la化合物及其鹽,其中!^係乙基,以及R3係氣 且其中A係選自基團A3.ccl至A3.cc81。 表323 :式la化合物及其鹽,其中ri、尺2及尺3係氫且其中a 係選自基團A3.cdl至A3.cd8 1。 表324 :式la化合物及其鹽,其中Ri係甲基,尺2及R3係氣 且其中A係選自基團A3.cdl至A3.cd81。 表325 :式la化合物及其鹽’其中ri係乙基,r2及r3係氣 且其中A係選自基團A3.cdl至A3.cd81。 133661.doc -86 - 200917962 表326 :式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中a 係選自基團八3^1至八3.〇681。 表327 :式la化合物及其鹽,其中尺]係曱基,尺2及尺3係氫 且其中A係選自基團A3.cel至A3.ce81。 表328 :式la化合物及其鹽,其中R〗係乙基,R2&amp;R3係氫 且其中A係選自基團A3.cei至A3.ce81。 表329 :式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中A 係選自基團A3.cfl至A3.cf81。 表330 :式la化合物及其鹽,其中Ri係甲基,…及尺3係氫 且其中A係選自基團A3.cfl至A3.cf81。 表331 :式la化合物及其鹽,其中Ri係乙基,…及尺3係氫 且其中A係選自基團A3.cfl至A3.cf81。 表332 :式la化合物及其鹽,其中Ri、尺2及尺3係氫且其中A 係選自基團A3.cgl至A3.cg8 1。 表333 :式la化合物及其鹽,其中Ri係曱基,尺2及尺3係氫 且其中A係選自基團A3 cgl至A3.cg81。 表334 :式la化合物及其鹽,其中Ri係乙基,尺2及尺3係氫 且其中A係選自基團A3.cgl至A3.cg81。 表335 :式la化合物及其鹽,其中r|、R2及R3係氫且其中A 係選自基團A3.chl至A3.ch81。 表336 :式la化合物及其鹽,其中R!係甲基,尺2及尺3係氫 且其中A係選自基團A3.chi至A3.ch81。 表337 :式la化合物及其鹽,其中Ri係乙基’以及尺3係氫 且其中A係選自基團A3.chi至A3.ch81。 133661.doc -87· 200917962 表338 :式la化合物及其鹽,其中R〗、R2及R3係氫且其中a 係選自基團A3.cil至A3.ci81。 表339 :式la化合物及其鹽,其中Ri係曱基,…及汉3係氣 且其中A係選自基團A3.cil至A3.ci81 〇 表340 :式la化合物及其鹽,其中R〗係乙基,以及尺3係氫 且其中A係選自基團A3.cil至A3.ci81。 表341 :式la化合物及其鹽,其中R!、R2及R3係氫且其中a 係選自基團A3.ckl至A3,ck81。 表342 :式la化合物及其鹽,其中Ri係曱基,…及汉3係氫 且其中A係選自基團A3.ckl至A3.ck81。 表343 :式la化合物及其鹽,其中R〗係乙基,…及汉3係氣 且其中A係選自基團A3.ckl至A3.ck81。 表344 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.cll至A3.C181。 表345 :式la化合物及其鹽’其中r1係曱基,R2及R3係氣 且其中A係選自基團A3.cll至A3.C181。 表346 :式la化合物及其鹽’其中Ri係乙基,尺2及R3係氫 且其中A係選自基團A3.cli至A3.C181。 表347 :式ia化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.cml至A3.cm81。 表348 :式la化合物及其鹽,其中R〗係甲基,尺2及R3係氫 且其中A係選自基團A3.cml至A3.cm81。 表349 :式Ia化合物及其鹽,其中Ri係乙基,尺2及R3係氫 且其中A係選自基團A3.cml至A3.cm81 〇 133661.doc -88- 200917962 表350 :式la化合物及其鹽,其中Rl、R2&amp;R3係氫且其中a 係選自基團A3.cnl至A3.cn81。 表351 :式la化合物及其鹽,其中Rl係甲基,…及汉3係氫 且其中A係選自基團A3.cnl至A3.cn81。 表352 :式la化合物及其鹽,其中Rl係乙基,“及…係氫 且其中A係選自基團A3 cnl至A3.cn81。 表353 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A3 _co 1至A3 .co8 1。 表354 :式la化合物及其鹽,其中Rl係曱基,R2及R3係氫 且其中A係選自基團A3.col至A3.co81 〇 表355 :式la化合物及其鹽,其中Ri ' R2及R3係氫且其中A 係選自基團A3.dal至A3.da81。 表3 56 :式la化合物及其鹽,其中Ri係甲基,R2及R3係氫 且其中A係選自基團A3.dal至A3.da81。 表3 57 :式la化合物及其鹽,其中Ri係乙基,R2&amp;R3係氫 且其中A係選自基團A3.dal至A3.da81。 表358 :式la化合物及其鹽,其中R1、尺2及R3係氫且其中A 係選自基團A3.dbl至A3.db81。 表3 59 :式la化合物及其鹽,其中R1係曱基,R2及R3係氣 且其中A係選自基團A3.dbl至A3.db81。 表360 :式la化合物及其鹽,其中R1係乙基,尺2及R3係氣 且其中A係選自基團A3.dbl至A3.db81。 表361 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A3 .dc 1至A3 .dc8 1。 133661.doc •89· 200917962 表362 :式la化合物及其鹽,其中Ri係甲基,R2及R3係氫 且其中A係選自基團A3.del至A3.dc81。 表363 :式la化合物及其鹽,其中R!係乙基,R2&amp;R3係氫 且其中A係選自基團A3.dcl至A3.dc81。 表364 :式la化合物及其鹽,其中Ri、尺2及R3係氫且其中A 係選自基團A3.ddl至A3.dd81。 表365 :式la化合物及其鹽’其中Ri係甲基,R2&amp;R3係氫 且其中A係選自基團A3.ddl至A3.dd81。 表366 :式la化合物及其鹽’其中R!係乙基,以及尺3係氫 且其中A係選自基團A3.ddl至A3.dd81。 表367 :式la化合物及其鹽,其中、R2&amp;R3係氫且其中A 係選自基團A3.del至A3.de81。 表3 68 :式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氫 且其中A係選自基團A3.del至A3.de81。 表3 69 :式la化合物及其鹽,其中R!係乙基,以及尺3係氣 且其中A係選自基團A3.del至A3.de81。 表3 70 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A3.dfl至A3.df81。 表371 :式la化合物及其鹽,其中R1係甲基,尺2及尺3係氣 且其中A係選自基團A3.dfl至A3.df81。 表3 72 :式la化合物及其鹽,其中R1係乙基,尺2及R3係氣 且其中A係選自基團A3.dfl至A3.df81。 表373 :式la化合物及其鹽’其中R1、R2及R3係氫且其中a 係選自基團A3.dgl至A3.dg81。 133661.doc -90- 200917962 表3 74 :式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氫 且其中A係選自基團A3.dgl至A3.dg81。 表375 :式la化合物及其鹽,其中Rl係乙基,“及汉3係氫 且其中A係選自基團A3.dgl至A3.dg81。 表376 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.dhl至A3.dh81。 表3 77 :式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氫 且其中A係選自基團A3.dhl至A3.dh81。 表378 :式la化合物及其鹽,其中Ri係乙基,…及尺3係氯 且其中A係選自基團A3.dhl至A3.dh81。 表379 :式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中a 係選自基團A3.dil至A3.di81。 表3 80 :式la化合物及其鹽,其中r/係甲基,R2&amp;R3係氫 且其中A係選自基團A3.dil至A3.di81。 表381 :式la化合物及其鹽,其中Ri係乙基,以及尺3係氣 且其中A係選自基團A3.dil至A3.di81。 表382 :式la化合物及其鹽,其中r1、R2&amp;R3係氫且其中A 係選自基團A3.dkl至A3.dk81。 表383 :式la化合物及其鹽,其中rJ係曱基,R2&amp;R3係氯 且其中A係選自基團A3.dkl至A3.dk81。 表3 84 :式la化合物及其鹽,其中係乙基,尺2及R3係氣 且其中A係選自基團A3.dk 1至A3.dk8 1。 表385 :式la化合物及其鹽’其中R1、尺2及R3係氫且其中A 係選自基團A3.dll至A3.dl81。 133661.doc -91 - 200917962 表3 86 :式la化合物及其鹽,其中…係甲基,R2&amp;R3係氫 且其中A係選自基團A3.dll至A3.dl81。 表387 :式la化合物及其鹽,其中Rl係乙基,R2&amp;R3係氣 且其中A係選自基團A3.dll至A3,dl81。 表388 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.dml至A3.dm8 1。 表389 :式la化合物及其鹽,其中!^係甲基,R2&amp;R3係氫 且其中A係選自基團A3 .dm 1至A3 .dm81。 表390 :式la化合物及其鹽,其中…係乙基,尺2及汉3係氫 且其中A係選自基團A3.dml至A3.dm81。 表391 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.dnl至A3.dn81。 表392 :式la化合物及其鹽,其中Ri係甲基,R2&amp;R3係氫 且其中A係選自基團A3 dnl至A3.dn81。 表393 :式la化合物及其鹽,其中Ri係乙基,R2&amp;R3係氮 且其中A係選自基團A3.dnl至A3.dn81。 表394 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.dol至A3.do81。 表395 :式la化合物及其鹽,其中…係曱基,…及汉3係氫 且其中A係選自基團A3.dol至A3.do81。 表396 :式la化合物及其鹽,其中Ri、R2AR3係氫且其中a 係選自基團A3,eal至A3.ea81。 表397 ·式la化合物及其鹽,其中r1係甲基,r2及r3係氫 且其中A係選自基團A3.eal至A3.ea81。 133661.doc -92- 200917962 表3 98 :式la化合物及其鹽,其中Ri係乙基,R2&amp;R3係氫 且其中A係選自基團A3.eal至A3.ea81。 表399 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.ebl至A3.eb81。 表400 :式la化合物及其鹽,其中R1係曱基,R2&amp;R3係氫 且其中A係選自基團A3.ebl至A3.eb81。 表401 :式la化合物及其鹽,其中Ri係乙基,以及尺3係氫 且其中A係選自基團A3.ebl至A3.eb81。 表402 :式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中a 係選自基團A3.ecl至A3.ec81。 表403 :式la化合物及其鹽,其中Ri係曱基,尺2及尺3係氫 且其中A係選自基團A3.eel至A3.ec81。 表404 :式la化合物及其鹽’其中Ri係乙基,R2&amp;R3係氫 且其中A係選自基團A3.eel至A3.ec81。 表405 :式la化合物及其鹽,其中R1、R2及R3係氫且其中a 係選自基團A3.edl至A3.ed81。 表406 :式la化合物及其鹽,其中Ri係甲基,R2及R3係氣 且其中A係選自基團A3.edl至A3.ed81。 表407 :式la化合物及其鹽’其中Ri係乙基,R2&amp;R3係氣 且其中A係選自基團A3.edl至A3.ed81。 表408 :式la化合物及其鹽,其中ri、R2&amp;R3係氫且其中A 係選自基團八3.661至八3.6681。 表409 :式la化合物及其鹽,其中Ri係曱基,R2及R3係氣 且其中A係選自基團A3.eel至A3.ee81。 133661.doc -93- 200917962 表 410 : 表 411 : 表 412 : 表 413 : 表 414 : 表 415 : 表 416 : 表 417 : 表 418 : 表 419 : 表 420 : 表 421 : 式la化合物及其鹽,其中Ri係乙基,R2及R3係氫 且其中A係選自基團A3.eel至A3.ee81。 式la化合物及其鹽,其中Ri、尺2及尺3係氫且其中a 係選自基團A3.efl至A3.ef8 1。 式la化合物及其鹽,其中Ri係曱基,…及尺3係氣 且其中A係選自基團A3.efl至A3.ef81。 式la化合物及其鹽,其中Ri係乙基,R2&amp;R3係氣 且其中A係遠自基團A3.efl至A3.ef81。 式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.egl至A3.eg81。 式la化合物及其鹽,其中R〗係甲基,尺2及尺3係氣 且其中A係選自基團A3.egl至A3.eg81。 式la化合物及其鹽,其中Ri係乙基,以及汉3係氫 且其中A係選自基團A3.egl至A3.eg81。 式la化合物及其鹽,其中Rl、R2&amp;R3係氫且其中a 係選自基團A3.ehl至A3.eh81。 式la化合物及其鹽,其中Ri係甲基,R2及R3係氫 且其中A係選自基團A3 ehl至A3.eh81。 式la化合物及其鹽,其中Rl係乙基,…及汉3係氫 且其中A係選自基團A3.ehl至A3.eh81。 式la化合物及其鹽,其中Ri、…及R3係氫且其中a 係選自基團A3.eil至A3.ei81。 式la化合物及其鹽,其中Ri係曱基,尺2及R3係氫 且其中A係選自基團A3.eil至A3.ei81。 133661.doc -94· 200917962 表 422 : 表 423 : 表 424 : 表 425 : 表 426 : 表 427 : 表 428 : 表 429 : 表 430 : 表 431 : 表 432 : 表 433 : 式la化合物及其鹽,其中R!係乙基,R2及R3係氫 且其中A係選自基團A3.eil至A3.ei81。 式la化合物及其鹽,其中Rl、…及尺3係氫且其中a 係選自基團A3.ekl至A3.ek81。 式la化合物及其鹽,其中Rl係甲基,尺2及尺3係氫 且其中A係選自基團A3.ekl至A3.ek81。 式la化合物及其鹽,其中Rl係乙基,尺2及尺3係氫 且其中A係選自基團A3.ekl至A3.ek81。 式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團八3.611至八3.〇181。 式la化合物及其鹽,其中R〗係甲基’ “及尺3係氫 且其中A係選自基團A3.ell至A3.el81。 式la化合物及其鹽’其中Ri係乙基,R2及R3係氫 且其中A係選自基團A3.ell至A3.el81。 式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.eml至A3.em8 1。 式la化合物及其鹽,其中…係甲基,尺2及尺3係氫 且其中A係選自基團A3.eml至A3.em81。 式la化合物及其鹽,其中Ri係乙基,R2&amp;R3係氫 且其中A係選自基團A3.ernl至A3.em81。 式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A3.enl至A3.en81。 式la化合物及其鹽,其中Ri係曱基,R2及r3係氫 且其中A係選自基團A3.enl至A3.en81。 133661.doc -95- 200917962 表434 :式la化合物及其鹽,其中R1係乙基,以及R3係氣 且其中A係選自基團A3.enl至A3.en81。 表435 :式la化合物及其鹽,其中r1、R2及R3係氫且其中a 係選自基團A3.eol至A3.eo81。 表436 :式la化合物及其鹽,其中R1係曱基,r2及R3係氣 且其中A係選自基團A3.eol至A3.eo81。 表437 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A3.fal至A3.fa81。 表438 :式la化合物及其鹽,其中R1係甲基,尺2及尺3係氮 且其中A係選自基團A3.fal至A3.fa81。 表439 :式la化合物及其鹽,其中R1係乙基,R2及R3係氮 且其中A係選自基團A3.fal至A3.fa81。 表440 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A3.fbl至A3.fb81。 表44 1 :式la化合物及其鹽,其中R1係甲基,R2及r3係氮 且其中A係選自基團A3.fbl至A3.fb81。 表442 :式la化合物及其鹽,其中R1係乙基,R2及r3係氯 且其中A係選自基團A3.fbl至A3.fb81。 表443 :式la化合物及其鹽,其中R1、R2及R3係氫且其中A 係選自基團A3.fcl至A3.fc81。 表444 :式la化合物及其鹽,其中R1係曱基,R2及r3係氣 且其中A係選自基團A3.fcl至A3.fc81。 表445 :式la化合物及其鹽,其中R1係乙基,R2&amp;R3係氣 且其中A係選自基團A3.fcl至A3.fc81。 133661.doc -96- 200917962 表446 :式la化合物及其鹽,其中Ri、R2&amp;R3係氫且其中a 係選自基團A3.fdl至A3.fd81。 表447 :式la化合物及其鹽,其中Ri係曱基,尺2及&amp;3係氣 且其中A係選自基團A3.fdl至A3.fd81。 表448 :式la化合物及其鹽,其中Ri係乙基,汉2及係氫 且其中A係選自基團A3.fdl至A3.fd81。 表449 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.fel至A3.fe81。 表450 :式la化合物及其鹽,其中Ri係甲基,…及尺3係氣 且其中A係選自基團A3.fel至A3.fe81。 表451 :式la化合物及其鹽,其中Ri係乙基,尺2及尺3係氫 且其中A係選自基團A3.fel至A3.fe81。 表452 :式la化合物及其鹽,其中、尺2及尺3係氫且其中A 係選自基團A3 . ff 1至A3. ff8 1。 表453 :式la化合物及其鹽,其中Ri係曱基,“及尺3係氫 且其中A係選自基團A3.ffl至A3.ff81。 表454 :式la化合物及其鹽,其中Ri係乙基,以及尺3係氫 且其中A係選自基團A3.ffl至A3.ff81。 表455 :式la化合物及其鹽,其中Ri、R2及R3係氫且其中A 係選自基團A3.fgl至A3.fg81。 表456 :式la化合物及其鹽,其中R〗係甲基,R2及R3係氫 且其中A係選自基團A3.fgl至A3.fg81。 表457 :式la化合物及其鹽,其中Ri係乙基,R2及R3係氫 且其中A係選自基團A3.fgl至A3.fg81。 133661.doc -97- 200917962 表 458 : 表 459 : 表 460 : 表 461 : 表 462 : 表 463 : 表 464 : 表 465 : 表 466 : 表 467 : 表 468 : 表 469 : 式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.fhl至A3.fh81。 式la化合物及其鹽,其中Ri係曱基,以及尺3係氣 且其中A係選自基團A3.fhl至A3.fh81。 式la化合物及其鹽’其中Ri係乙基,…及尺3係氣 且其中A係選自基團A3.fhl至A3.fh81。 式la化合物及其鹽,其中Ri、…及尺3係氫且其中a 係選自基團Α3.Π1至Α3.Π81。 式la化合物及其鹽’其中Ri係甲基,“及尺3係氣 且其中A係選自基團A3.fi 1至A3.Π81。 式la化合物及其鹽,其中R〗係乙基,“及尺3係氣 且其中A係選自基團A3.fil至A3.fi81。 式la化合物及其鹽,其中Ri、R2及R3係氫且其中a 係選自基團A3.fkl至A3.fk81。 式la化合物及其鹽,其中R】係曱基,反2及反3係氣 且其中A係選自基團A3.fkl至A3.fk81。 式la化合物及其鹽,其中係乙基,R2及R3係氣 且其中A係選自基團A3.fkl至A3.fk81。 式la化合物及其鹽,其中Ri、…及反3係氫且其中a 係選自基團A3.fll至Α3.Π8 1。 式la化合物及其鹽,其中係曱基,R2&amp;R3係氣 且其中A係選自基團A3.fll至A3.fl81。 式la化合物及其鹽’其中Ri係乙基,尺2及R3係氣 且其中A係選自基團A3.fll至A3.fl81。 133661.doc -98- 200917962 表470 :式la化合物及其鹽’其中Ri、R2及R3係氫且其中a 係選自基團A3.fml至A3.fm81。 表471 :式la化合物及其鹽,其中Ri係曱基,以及汉3係氣 且其中A係選自基團A3.fml至A3.fm81。 表472 :式la化合物及其鹽’其中Ri係乙基,以及尺3係氣 且其中A係選自基團A3.fml至A3.fm81。 表473 :式la化合物及其鹽,其中R!、尺2及R3係氫且其中a 係選自基團A3.fnl至A3.fn81。 f 表474 :式la化合物及其鹽,其中Ri係甲基,尺2及汉3係氣 且其中A係選自基團A3.fnl至A3.fn81。 表475 :式la化合物及其鹽,其中Ri係乙基,“及汉3係氣 且其中A係選自基團A3.fnl至A3.fn81。 表476 :式la化合物及其鹽,其中Rl、R2及R3係氫且其中a 係選自基團A3.f〇l至A3.fo81。 表477 .式la化合物及其鹽,其中Ri係曱基’尺2及r3係氫 且其中A係選自基團A3.fol至A3.f〇81。 式I或II化合物可藉由有機化學之標準方法來製備,例如 藉由下文或工作實例中所述之方法來製備: 其中X為〇且X3為孤電子對之Si化合物可根據(例如)方 案1中所繪示之方法藉由使經活化。比讀㈣生物Π與3_胺 基吡啶化合物m反應來製備(參見例如Houben_we汁 &quot;Methoden Chemistry] der organ. Chemie&quot; [Methods 〇f 〇rganic Georg-Thieme-Verlag, Stuttgart, New York 經活化α比唾叛酸衍生物Π 1985,第 E5卷,第 941_1〇45頁 133661.doc •99- 200917962 係(例如)函化物、活化酿、酸針、4氮化物,例如氯化 物、氟化物、溴化物、對硝基苯基酯、五氟苯基酯 ' 冰羥 基琥珀醯亞胺、羥基苯并三唑基酯。在方案工中,基: A R R及R具有上述含義且尤其具有所述較佳含義, X係適宜離去基團,例如_素、%、^肖^ 苯氧基等。 &lt; 方案1 : A、 ΟΙ)Table 79: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Abl to A2. Ab81. Table 80: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, R2 and R3 are a gas and wherein A is selected from the group A2. Abl to A2. Ab81. 133661. Doc-65- 200917962 Table 81: Compounds of the formula la and salts thereof, wherein Ri is ethyl and 3 is gas and wherein A is selected from the group A2. Abl to A2. Ab81. Table 82: Compounds of the formula la and salts thereof, wherein r1, R2 and R3 are hydrogen and wherein a is selected from the group A2. Acl to A2. Ac81. Table 83: Compounds of the formula la and salts thereof, wherein R1 is methyl, R2&amp;R3 is hydrogen and wherein A is selected from the group A2. Acl to A2. Ac81. Table 84: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2&amp;R3 is a gas and wherein A is selected from the group A2. Acl to A2. Ac81. Table 85: Compounds of the formula la and salts thereof, wherein r1, R2 and R3 are hydrogen and wherein A is selected from the group A2, adl to A2. Ad81. Table 86: Compounds of the formula la and salts thereof, wherein R1 is methyl, and amphibious 3 is gas and wherein A is selected from the group A2. Adl to A2. Ad81. Table 87: Compounds of the formula la and salts thereof, wherein R1 is ethyl, 1^2 and R3 are gaseous and wherein A is selected from the group A2. Adl to A2. Ad81. Table 88: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Ael to A2. Ae81. Table 89: Compounds of the formula la and salts thereof, wherein R1 is methyl, R2 and R3 are gaseous and wherein A is selected from the group A2. Ael to A2. Ae81. Table 90: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2 and R3 are gaseous and wherein A is selected from the group A2. Ael to A2. Ae81. Table 91: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Afl to A2. Af81. Table 92: Compounds of the formula la and salts thereof, wherein R1 is methyl, R2 and R3 are gaseous and wherein A is selected from the group A2. Afl to A2. Af81. I33661. Doc-66- 200917962 Table 93: Compounds of the formula la and salts thereof, wherein W is ethyl, sizing 2 and R3 are gaseous and wherein A is selected from the group A2. Afl to A2. Af81. Table 94: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Agl to A2. Ag81. Table 95: Compounds of the formula la and salts thereof, wherein R1 is methyl, R2 and R3 are gaseous and wherein A is selected from the group A2. Agl to A2. Ag81. Table 96: Compounds of the formula la and salts thereof, wherein R1 is ethyl and 3 is gas and wherein A is selected from the group A2. Ahl to A2. Ah81. Table 97: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Ail to A2. Ai81. Table 98: Compounds of the formula la and salts thereof, wherein R1 is a methyl group, and a genus 3 is a gas and wherein the A is selected from the group A2. Ail to A2. Ai81. Table 99: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2&amp;R3 is a gas and wherein the A is far from the group A2. Ail to A2. Ai81. Table 100: Compounds of the formula la and salts thereof, wherein R1, R2 &amp; R3 are hydrogen and wherein A is selected from the group A2. Akl to A2. Ak81. Table 101: Compounds of the formula la and salts thereof, wherein R is a fluorenyl group, and a sulphate is a hydrogen group and wherein the A group is selected from the group A2. Akl to A2. Ak81. Table 102: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2&amp;R3 is hydrogen and wherein A is selected from the group A2. Akl to A2. Ak81. Table 103: Compounds of the formula la and salts thereof, wherein Ri, ... and 3 are hydrogen and wherein A is selected from the group A2. All to A2. Al81. Table 104: Compounds of the formula la and salts thereof, wherein ... are methyl, R2 and R3 are hydrogen and wherein A is selected from the group A2. All to A2. Al81. 133661. Doc-67- 200917962 Table 105: Compounds of the formula la and salts thereof, wherein R1 is ethyl, sizing 2 and R3 are hydrogen and wherein A is selected from the group A2. All to A2. Al81. Table 106: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Aml to A2. Am81. Table 107: Compounds of the formula la and salts thereof, wherein R1 is methyl, r2 and R3 are gaseous and wherein A is selected from the group A2. Aml to A2. Am81. Table 1 08: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2 and R3 are gaseous and wherein A is selected from the group A2. Aml to A2. Am81. Table 109: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Anl to A2. An81 〇 Table 110: Compounds of the formula la and salts thereof, wherein R1 is methyl, R2 and R3 are hydrogen and wherein A is selected from the group A2. Anl to A2. An81. Table 1 : a compound of the formula la and a salt thereof, wherein R1 is an ethyl group, R2 and r3 are a gas and wherein A is selected from the group A2. Anl to A2. An81 〇 Table 112: a compound of the formula la and a salt thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Aol to A2. Ao81. Table 11 3: a compound of the formula la and a salt thereof, wherein R1 is a methyl group, R2 and R3 are hydrogen and wherein A is selected from the group A2. Aol to A2. Ao81. Table 114: Compounds of the formula la and salts thereof, wherein R1 is ethyl, ft 2 and R3 are gaseous and wherein A is selected from the group A2. Aol to A2. Ao81. Table U 5 : a compound of the formula la and a salt thereof, wherein r1, R2 and R3 are hydrogen and wherein a is selected from the group A2. Bal to A2. Ba81. Table 116: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 &amp; R3 is gaseous and wherein A is selected from the group A2. Bal to A2. Ba81. 133661. Doc-68- 200917962 Table 1 17: Compounds of the formula la and salts thereof, wherein Ri is ethyl, sizing 2 and R3 are hydrogen and wherein A is selected from the group A2. Bal to A2. Ba81. Table 118: Compounds of the formula la and salts thereof, wherein r1 '2 and R3 are hydrogen and wherein A is selected from the group A2. Bbl to A2. Bb81. Table 119: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 and R3 are hydrogen and wherein A is selected from the group A2. Bbl to A2. Bb81. Table 120: Compounds of the formula la and salts thereof, wherein r1 is ethyl, R2 and R3 are hydrogen and wherein A is selected from the group A2. Bbl to A2. Bb81. Table 121: Compounds of the formula la and salts thereof, wherein ri, ulmen 2 and R3 are hydrogen and wherein a is selected from the group A2. Bcl to A2. Bc81. Table 122: Compounds of the formula la and salts thereof, wherein Ri is methyl, sizing 2 and R3 are hydrogen and wherein A is selected from the group A2. Bcl to A2. Bc81. Table 123: Compounds of the formula la and salts thereof, wherein Ri is ethyl, sizing 2 and R3 are hydrogen and wherein A is selected from the group A2. Bcl to A2. Bc81. Table 124: Compounds of the formula la and salts thereof, wherein ri, R2 and R3 are hydrogen and wherein A is selected from the group A2. Bdl to A2. Bd81. Table 125: Compounds of the formula la and salts thereof, wherein r1 is methyl, r2 and R3 are nitrogen and wherein A is selected from the group A2. Bdl to A2. Bd81. Table 126: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 and R3 are hydrogen and wherein A is selected from the group A2. Bdl to A2. Bd81. Table 127: Compounds of the formula la and salts thereof, wherein r', R2 and R3 are hydrogen and wherein A is selected from the group A2. Bel to A2. Be81. Table 128: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, R2 and R3 are hydrogen and wherein A is selected from the group A2. Bel to A2. Be81. 133661. Doc-69- 200917962 Table 129: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A2. Bel to A2. Be81. Table 130: Compounds of the formula la and salts thereof, wherein Ri, Ruler 2 and Rule 3 are hydrogen and wherein a is selected from the group A2. Bfl to A2. Bf81. Table 131: Compounds of the formula la and salts thereof, wherein R is methyl, the quaternary 2 and R3 are hydrogen and wherein the A is selected from the group A2. Bfl to A2. Bf81. Table 132: Compounds of the formula la and salts thereof, wherein Ri is ethyl, sizing 2 and R3 are hydrogen and wherein A is selected from the group A2. Bfl to A2. Bf81. Table 133: Compounds of the formula la and salts thereof, wherein Ri, ... and 3 are hydrogen and wherein A is selected from the group A2. Bgl to A2. Bg81. Table 134: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, the sizing elements 2 and R3 are hydrogen and wherein the A group is selected from the group A2. Bgi to A2. Bg81. Table 135: Compounds of the formula la and salts thereof, wherein Ri is ethyl, sizing 2 and sizing 3 are hydrogen and wherein A is selected from the group A2. Bhl to A2. Bh8 1. Table 136: Compounds of the formula la and salts thereof, wherein Ri, Ruler 2 and Rule 3 are hydrogen and wherein A is selected from the group A2. Bil to A2. Bi81. Table 137: Compounds of the formula la and salts thereof, wherein are fluorenyl, R2 &amp; R3 are hydrogen and wherein A is selected from the group A2. Bil to A2. Bi81. Table 138: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 and R3 are hydrogen and wherein A is selected from the group A2. Bil to A2. Bi81. Table 139: Compounds of the formula la and salts thereof, wherein R, R2 &amp; R3 are hydrogen and wherein a is selected from the group A2. Bkl to A2. Bk81. Table 140: Compounds of the formula la and salts thereof, wherein Ri is methyl, and amp 3 is hydrogen and wherein A is selected from the group A2. Bkl to A2. Bk81. 133661 . Doc-70- 200917962 Table 14 1 : Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2 and r3 are gas and wherein A is selected from the group A2. Bkl to A2. Bk81. Table 142: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Bll to A2. Bl81. Table 143: Compounds of the formula la and salts thereof, wherein R1 is a methyl group, and a genus 3 is a gas and wherein the A is selected from the group A2. Bll to A2. M81. Table 144: Compounds of the formula la and salts thereof, wherein are ethyl, R2 &amp; R3 gas and wherein A is selected from the group A2. M1 to A2. Bl81. Table 145: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Bml to A2. Bm81. Table 146: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, R2 and R3 are a gas and wherein A is selected from the group A2. Bml to A2, bm81. Table 147: Compounds of the formula la and salts thereof, wherein R1 is ethyl, r2 and R3 are gaseous and wherein A is selected from the group A2. Bml to A2. Bm81. Table 148: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A2, bnl to A2. Bn81. Table 149: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, R2 and R3 are chloro and wherein A is selected from the group A2. Bnl to A2. Bn81. Table 150: Compounds of the formula la and salts thereof, wherein r is ethyl, R2 &amp; R3 is gaseous and wherein A is selected from the group A2. Bnl to A2. Bn81. Table 151: Compounds of the formula la and salts thereof, wherein r], r2&amp;r3 are hydrogen and wherein A is selected from the group A2. Bol to A2. Bo81. Table 152: Compounds of the formula la and salts thereof, wherein R1 is methyl, R2 and R3 are gaseous and wherein A is selected from the group A2. Bol to A2. Bo81. 133661. Doc 200917962 Table 153: Table 154: Table 155: Table 156: Table 157: Table 158: Table 159: Table 160: Table 161: Table 162: Table 163: Table 164: Compounds of the formula la and salts thereof, wherein are ethyl, R2 and R3 are gas and wherein A is selected from the group A2. Bol to A2. Bo81. a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A2. Cal to A2. Ca81. a compound of the formula la and a salt thereof, wherein Ri is a methyl group, R2&amp;R3 is a gas and wherein A is selected from the group A2. Cal to A2. Ca81. a compound of the formula la and a salt thereof, wherein Ri is an ethyl group, and a Han 3 gas and wherein the A group is selected from the group A2. Cal to A2. Ca81. a compound of the formula la and a salt thereof, wherein Ri, ... and 3 are hydrogen and wherein a is selected from the group A2. Cbl to A2. Cb81. a compound of the formula la and a salt thereof, wherein Ri is a fluorenyl group, and a calilem 3 is hydrogen and wherein A is derived from the group A2. Cb 1 to A2. Cb8 1. a compound of the formula la and a salt thereof, wherein Ri is an ethyl group, and a calilem 3 gas and wherein the A group is selected from the group A2. Cbl to A2. Cb81. a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A2. Ccl to A2. Cc81. a compound of the formula la and a salt thereof, wherein Ri is a fluorenyl group, R2 &amp; R3 is hydrogen and wherein A is selected from the group A2. Cc 1 to A2. Cc81. a compound of the formula la and a salt thereof, wherein R is ethyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A2. Ccl to A2. Cc81. A compound of the formula 1a and a salt thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Cdl to A2. Cd81. a compound of the formula la and a salt thereof, wherein Ri is a methyl group, R2&amp;R3 is a gas and wherein A is selected from the group A2. Cdl to A2. Cd81. 133661. Doc-72- 200917962 Table 165: Compounds of the formula la and salts thereof, wherein Ri is ethyl, sizing 2 and sizing 3 are hydrogen and wherein A is selected from the group A2. Cdl to A2. Cd81. Table 166: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A2. Cel to A2. Ce81. Table 167: Compounds of the formula la and salts thereof, wherein Ri is methyl, sizing 2 and R3 are hydrogen and wherein A is selected from the group A2. Cel to A2. Ce81. Table 168: Compounds of the formula la and salts thereof, wherein Ri is ethyl, "and the rule 3 is chlorine and wherein the A is selected from the group A2. Cel to A2. Ce81. Table 169: Compounds of the formula la and salts thereof, wherein Ri, ... and 3 are hydrogen and wherein A is selected from the group A2. Cfl to A2. Cf81. Table 170: Compounds of the formula la and salts thereof, wherein Ri is methyl, ... and 3 is hydrogen and wherein A is selected from the group A2. Cfl to A2. Cf81. Table 171: Compounds of the formula la and salts thereof, wherein Ri is ethyl, ... and Han 3 gas and wherein A is selected from the group A2. Cfl to A2. Cf81. Table 172: Compounds of the formula la and salts thereof, wherein Ri, Ruler 2 and Rule 3 are hydrogen and wherein a is selected from the group A2. Cgl to A2. Cg81. Table 173: Compounds of the formula la and salts thereof, wherein Ri is a sulfhydryl group, a ft 2 and a Han 3 nitrogen and wherein the A is selected from the group A2. Cgl to A2. Cg81. Table 174: Compounds of the formula la and salts thereof, wherein Ri is ethyl, sizing 2 and R3 are chlorine and wherein A is selected from the group A2. Chl to A2. Ch81. Table 175: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A2, cil to A2. Ci81. Table 176: Compounds of the formula la and salts thereof, wherein Ri is methyl, ft 2 and R3 are nitrogen and wherein A is selected from the group A2. Cil to A2. Ci81. 133661. Doc-73- 200917962 Table 177: Compounds of the formula la and salts thereof, wherein Ri is ethyl, sizing 2 and R3 are hydrogen and wherein A is selected from the group A2. Cil to A2. Ci81. Table 178: Compounds of the formula la and salts thereof, wherein r1, R2 and R3 are hydrogen and wherein a is selected from the group A2. Ckl to A2. Ck81. Table 179: Compounds of the formula la and salts thereof, wherein R1 is methyl, R2&amp;R3 is hydrogen and wherein A is selected from the group A2. Ckl to A2. Ck81. Table 180: Compounds of the formula la and salts thereof, wherein R1 is ethyl, ft 2 and R3 are gaseous and wherein A is selected from the group A2. Ckl to A2. Ck81. Table 181: Compounds of the formula la and salts thereof, wherein r1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Cll to A2. Cl81. Table 182: Compounds of the formula la and salts thereof wherein R! is a fluorenyl group, a sizing element 2 and an R3 group are chlorine and wherein the A group is selected from the group A2. Cll to A2. C181. Table 183: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2&amp;R3 is a gas and wherein A is selected from the group A2. Cll to A2. C181. Table 184: a compound of the formula la and a salt thereof wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A2. Cml to A2. Cm81. Table 185: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, R2 and R3 are a gas and wherein the A group is selected from the group A2. Cml to A2. Cm81. Table 186: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2 and R3 are gaseous and wherein A is selected from the group A2. Cml to A2. Cm81. Table 187: Compounds of the formula la and salts thereof, wherein r1, R2 and R3 are hydrogen and wherein a is selected from the group A2. Cnl to A2. En81. Table 1 8 8 : a compound of the formula la and a salt thereof, wherein Ri is a methyl group, R 2 and R 3 are a gas and wherein A is selected from the group A 2 . Cnl to A2. Cn81. 133661. Doc •74- 200917962 Table 189: Compounds of formula la and their salts' wherein r1 is ethyl, Han 2 and R 3 are gases and wherein A is selected from group A2. Cnl to A2. Cn81. Table 190: Compounds of the formula la and salts thereof, wherein r, r2 and R3 are hydrogen and wherein a is selected from the group A2. Col to A2. Co81. Table 191: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, R2&amp;R3 is a gas and wherein A is selected from the group A2. Col to A2. Co81. Table 192: Compounds of the formula la and salts thereof, wherein Ri is ethyl and 3 is gas and wherein A is selected from the group A2. Co 1 to A2. Co8 1. Table 193: Compounds of the formula la and salts thereof, wherein Ri, Ruler 2 and R3 are hydrogen and wherein a is selected from the group A2. Dal to A2. Da81. Table 194: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A2. Dal to A2. Da81. Table 195: Compounds of the formula la and salts thereof, wherein R] is ethyl, R2&amp;R3 is a gas and wherein A is selected from the group A2. Dal to A2. Da81. Table 196: Compounds of the formula la and salts thereof, wherein Ri, R2 &amp; R3 are hydrogen and wherein A is selected from the group A2. Dbl to A2. Db81. Table 197: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, R2 and R3 are hydrogen and wherein A is selected from the group A2. Dbl to A2. Db81. Table 198: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A2 to A2. Db81. Table 199: Compounds of the formula la and salts thereof, wherein Ri, R2 &amp; R3 are hydrogen and wherein A is selected from the group A2. Dcl to A2. Dc81. Table 200: Compounds of the formula la and salts thereof, wherein Ri is methyl, sizing 2 and R3 are hydrogen and wherein A is selected from the group A2. Dcl to A2. Dc81. 133661. Doc-75- 200917962 Table 201: Table 202: Table 203: Table 204: Table 205: Table 206: Table 207: Table 208: Table 209 · Table 210: Table 211: Table 212: Compounds of Formula la and their salts R1 is ethyl, 尺 2 and R3 are chlorine and wherein A is selected from the group A2. Dcl to A2. Dc81. a compound of the formula la and a salt thereof wherein R, R2 and R3 are hydrogen and wherein A is selected from the group A2. Ddl to A2. Dd81. a compound of the formula la and a salt thereof, wherein R is a methyl group, and a calilem 3 is ammonia and wherein the A group is selected from the group A2. Ddl to A2. Dd81. a compound of the formula la and a salt thereof, wherein r is ethyl, R2 &amp; R3 is a gas and wherein A is selected from the group A2. Ddl to A2. Dd81. a compound of the formula la and a salt thereof, wherein r1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Del to A2. De81. a compound of the formula la and a salt thereof, wherein the methyl group, and the calilem 3 are hydrogen and wherein the A group is selected from the group A2. Del to A2. De81. a compound of the formula la and a salt thereof, wherein Ri is ethyl, and 3 is chlorine and wherein A is selected from the group A2. Del to A2. De81. a compound of the formula la and a salt thereof, wherein Ri, R2 &amp; R3 are hydrogen and wherein A is selected from the group A2. Dfl to A2. Df81. a compound of the formula la and a salt thereof, wherein Ri is a fluorenyl group, a sizing element 2 and a sizing element 3 are hydrogen and wherein the A group is selected from the group A2. Dfl to A2. Df81. a compound of the formula la and a salt thereof, wherein Ri is ethyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A2. Dfl to A2. Df81. a compound of the formula la and a salt thereof, wherein R 2 and R 3 are hydrogen and wherein A is selected from the group A 2 . Dgl to A2. Dg81. A compound of the formula 1a and a salt thereof, wherein R is a fluorenyl group, R2 and R3 are hydrogen and wherein A is selected from the group A2. Dgl to A2. Dg81. 133661. Doc-76- 200917962 Table 213: Compounds of the formula la and salts thereof, wherein R] is ethyl, R2&amp;R3 is gaseous and wherein A is selected from the group A2. Dhl to A2. Dh81. Table 214: Compounds of the formula la and salts thereof, wherein Ri, R2 &amp; R3 are a gas and wherein a is selected from the group A2. Dil to A2. Di81. Table 215: Compounds of the formula la and salts thereof, wherein Ri is methyl 'R2&amp; R3 is hydrogen and wherein A is selected from the group A2. Dil to A2. Di81. Table 216: Compounds of the formula la and salts thereof, wherein Ri is ethyl and 3 is gas and wherein A is selected from the group A2. Dil to A2. Di81. Table 217: Compounds of the formula 1a and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A2. Dkl to A2. Dk81. Table 218: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A2. Dkl to A2. Dk81. Table 219: Compounds of the formula la and salts thereof, wherein Ri is an ethyl group, and a genus 3 is a gas and wherein the A group is selected from the group A2. Dkl to A2. Dk81. Table 220: a compound of the formula la and a salt thereof, wherein Ri, the ruler 2 and the ruler 3 are hydrogen and wherein a is selected from the group A2. Dll to A2. Dl81. Table 221: Compounds of the formula 13 and salts thereof, wherein 111 is methyl, 112 and 113 are hydrogen and wherein A is selected from the group A2. Dll to A2. Dl81. Table 222: Compounds of the formula la and salts thereof, wherein Ri is ethyl, and Han 3 is hydrogen and wherein A is selected from the group A2. Dll to A2. Dl81. Table 223: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A2. Dml to A2. Dm81. Table 224: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A2. Dml to A2. Dm81. 133661. Doc -77- 200917962 Table 225 Table 226 Table 227 Table 228 ('Table 229 Table 230 Table 231 Another A \ R1 R2 R3 : a compound of the formula la and a salt thereof, wherein Ri is an ethyl group, R 2 &amp; R 3 is hydrogen and wherein A Is selected from the group A2. Dml to A2. Dm81. And a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A2. Dnl to A2. Dn81. A compound of the formula la and a salt thereof, wherein Ri is methyl, and 3 is hydrogen and wherein A is selected from the group VIII (1111 to VIII). (11181. A compound of the formula la and a salt thereof, wherein Ri is ethyl, R2&amp; R3 is hydrogen and wherein A is selected from the group A2. Dnl to A2. Dn81. a compound of the formula la and a salt thereof, wherein Ri, R2 &amp; R3 are hydrogen and wherein a is selected from the group A2. Dol to A2. Do81. A compound of the formula la and a salt thereof, wherein Ri is a fluorenyl group, "and a dentate 3 is hydrogen and wherein the A is selected from the group A2. Dol to A2. Do81. And a salt thereof, wherein R is ethyl, R2 and R3 are hydrogen and wherein A is selected from the group A2. Dol to A2, do81. A preferred embodiment is a compound of the formula la and a salt thereof, wherein the group A3' as defined herein is especially a group A3 wherein r43, r53 and R63 have the preferred meanings, especially the formula VIII3(10) to A3. Pyrazolyl of do, for example selected from pyrazolyl A3 aal_A3旳81 to A3. dol-A3. a group of do81; hydrogen, C丨-CV alkyl or Cl_C4_alkoxy·CpC2·alkyl, most preferably hydrogen, methyl or ethyl; selected from hydrogen, methyl, difluoromethyl, Trifluoromethyl, decyloxy, di-haloxycarbonyl and trifluoromethoxy; and is selected from the group consisting of hydrogen, methyl, difluoromethyl, trifluoromethyl, methoxy 133661. Doc-78- 200917962, difluoromethoxy and trifluoromethoxy; and wherein one or both of the groups... and R3 are hydrogen. Examples of the compounds of this preferred embodiment are the compounds listed in Table 2 below; 32 to 477. Table 232: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A3. Aal to A3. Aa81. Table 233: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Aal to A3. Aa81. Table 234: Compounds of the formula la and salts thereof, wherein R is ethyl, R2 and R3 are hydrogen and wherein A is selected from the group A3. Aal to A3. Aa81. Table 235: Compounds of the formula la and salts thereof, wherein R!, R2 and R3 are hydrogen and wherein a is selected from the group A3. Abl to A3. Ab81. Table 236: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, and the genus 3 is hydrogen and wherein the A group is selected from the group A3, abl to A3. Ab81. Table 237: Compounds of the formula la and salts thereof, wherein Ri is ethyl, and 3 is hydrogen and wherein A is selected from the group A3. Abl to A3. Ab81. Table 238: Compounds of the formula la and salts thereof, wherein R2 and R3 are hydrogen and wherein a is selected from the group A3. Acl to A3. Ac81. Table 239: Compounds of the formula la and salts thereof, wherein Ri is methyl, and amp 3 is hydrogen and wherein A is selected from the group A3. Acl to A3. Ac81. Table 240: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 and R3 are hydrogen and wherein A is selected from the group A3. Acl to A3. Ac81. Table 241: Compounds of the formula la and salts thereof, wherein Ri, and Caliper 3 are hydrogen and wherein a is selected from the group A3, adl to A3. Ad81. 133661. Doc •79- 200917962 Table 242: Compounds of the formula la and their salts, in which Ri is methyl, Han 2 and R 3 are hydrogen and wherein A is selected from the group A3. Adl to A3. Ad81. Table 243: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 and R3 are chlorine and wherein A is selected from the group A3. Adl to A3. Ad81. Table 244: Compounds of the formula la and salts thereof, wherein ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Ael to A3. Ae8 1. Table 245: Compounds of the formula la and salts thereof, wherein Ri is methyl, and R3 is hydrogen and wherein A is selected from the group A3. Ael to A3. Ae81. Table 246: Compounds of the formula la and salts thereof, wherein Ri is ethyl, sizing 2 and sizing 3 are hydrogen and wherein A is selected from the group A3. Ael to A3. Ae81. Table 247: Compounds of the formula la and salts thereof, wherein ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Afl to A3. Af81. Table 248: Compounds of the formula la and salts thereof, wherein Ri is methyl, ... and Han 3 hydrogen and wherein A is selected from the group A3. Ai l to A3. Af81. Table 249: Compounds of the formula la and salts thereof, wherein Ri is ethyl, ft 2 and Han 3 hydrogen and wherein A is selected from the group A3. Afl to A3. Af81. Table 250: a compound of the formula la and a salt thereof, wherein Ri, the ruler 2 and the rule 3 are hydrogen and wherein a is selected from the group A3. Agl to A3. Ag81. Table 251: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, ... and a Han 3 series hydrogen and wherein the A group is remote from the group A3. Agl to A3. Ag81. Table 252: Compounds of the formula la and salts thereof, wherein R1 is ethyl, ... and Han 3 hydrogen and wherein A is selected from the group A3. Agl to A3. Ag81. Table 253: Compounds of the formula la and salts thereof, wherein Ri, Ruler 2 and Rule 3 are hydrogen and wherein a is selected from the group A3. Ahl to A3. Ah81. 133661. Doc -80- 200917962 Table 254: Table 255: Table 256: Table 257: Table 258: Table 259: Table 260: Table 261: Table 262: Table 263: Table 264: Table 265: Formula la compounds and salts thereof, wherein Rl Is a methyl group, R2 and R3 are hydrogen and wherein A is selected from the group A3. Ahl to A3. Ah81. a compound of the formula la and a salt thereof, wherein is an ethyl group, R2 and R3 are hydrogen and wherein A is selected from the group A3. Ahl to A3. Ah81. A compound of the formula 1a and a salt thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group VIII. &amp; 丨 1 to 八 3 meaning 81. a compound of the formula la and a salt thereof, wherein Ri is a sulfhydryl group, a ruthenium 2 and a Han 3 gas, and wherein the A is distant from the group A3. Ail to A3. Ai81. a compound of the formula la and a salt thereof, wherein R] is an ethyl group, R2 and R3 are a gas and wherein the A group is selected from the group consisting of a group A3, ail to A3. Ai81. a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A3. Akl to A3. Ak81. a compound of the formula la and a salt thereof, wherein Ri is a methyl group, the rule 2 and the rule 3 are hydrogen and wherein the A is selected from the group A3. Akl to A3. Ak81. a compound of the formula la and a salt thereof, wherein Ri is an ethyl group, and a genus 3 is hydrogen and wherein the A group is selected from the group A3. Akl to A3. Ak81. a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A3. All to A3. Al81. a compound of the formula la and a salt thereof, wherein Ri is a fluorenyl group, the quaternary 2 and the R 3 are hydrogen and wherein the A is selected from the group A3. All to A3. Al81. a compound of the formula la and a salt thereof wherein R is an ethyl group, a Han 2 and an R 3 are hydrogen and wherein the A group is selected from the group A3. All to A3. Al81. a compound of the formula la and a salt thereof, wherein R1, 尺2 and R3 are hydrogen and wherein A is selected from the group VIII. Strong 1111 to 8 3. 311181. I33661. Doc-81 - 200917962 Table 266: Table 267: Table 268: Table 269: Table 270: Table 271: Table 272: Table, 273: Table 274: Table 275: Table 276: Table 277: Compounds of the formula la and their salts, wherein Rl is a methyl group, and a Han 3 gas and wherein the A is selected from the group A3. Aml to A3. Am81. The compound of the formula la and its salt' are in the form of an ethyl group, and a genus of the genus 3 and wherein the group A is selected from the group A3. Am 1 to A3, am8 1. a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Anl to A3. An81. a compound of the formula la and a salt thereof, wherein R1 is a fluorenyl group, and a sulphate 3 system gas and wherein the A group is selected from the group A3. Anl to A3. An81. a compound of the formula la and a salt thereof, wherein Ri is an ethyl group, a ruthenium 2 and a R3 system gas, and wherein the A group is selected from the group A3. Anl to A3. An81. a compound of the formula la and a salt thereof, wherein R, ... and 3 are hydrogen and wherein a is selected from the group A3. Aol to A3. Ao81. a compound of the formula la and a salt thereof, wherein ... is a methyl group, a dentine 2 and a genus 3 is hydrogen and wherein the A is distant from the group A^. Aol to A3. Ao81. a compound of the formula la and a salt thereof, wherein R, "and R3 are hydrogen and wherein a is selected from the group A3. Bal to A3. Ba81. a compound of the formula la and a salt thereof, wherein Ri is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Bal to A3. Ba81. A compound of the formula la and a salt thereof wherein Ri is an ethyl group, R2 and R3 are hydrogen and wherein A is selected from the group A3. Bal to A3. Ba81. a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A3. Bbl to A3. Bb81. a compound of the formula la and a salt thereof, wherein Ri is a methyl group, and a striate 3 is hydrogen and wherein the A is selected from the group A3. Bbl to A3. Bb81. 133661. Doc-82- 200917962 Table 278: Table 279: Table 280: Table 281: Table 282: Table 283: Table 284: Table 285: Table 286: Table 287: Table 288: Table 289: Compounds of the formula la and their salts, wherein Ri Is an ethyl group, and a genus 3 gas and wherein A is selected from the group A3. Bbl to A3. Bb81. a compound of the formula la and a salt thereof, wherein r1, r2 and R3 are hydrogen and wherein A is selected from the group A3. Bcl to A3. Bc81. a compound of the formula la and a salt thereof, wherein Ri is a methyl group, and a calilem 3 is a gas and wherein the A is selected from the group A3. Bcl to A3. Bc81. a compound of the formula la and a salt thereof, wherein is an ethyl group, and a Han 3 gas and wherein the A group is selected from the group A3. Bci to A3. Bc81. a compound of the formula la and a salt thereof wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Bdl to A3. Bd81. And a salt thereof, wherein Ri is a methyl group, R2 and R3 are a gas and wherein A is selected from the group A3. Bdl to A3. Bd81. a compound of the formula la and a salt thereof, wherein is an ethyl group, R2&amp;R3 is a gas and wherein A is selected from the group A3. Bdl to A3. Bd81. a compound of the formula la and a salt thereof, wherein Ri, and the rule 3 are hydrogen and wherein a is selected from the group A3. Bel to A3. Be81. And a salt thereof, wherein Ri is a fluorenyl group, R2 and R3 are a gas and wherein A is selected from the group A3. Bel to A3. Be81. a compound of the formula la and a salt thereof, wherein Ri is an ethyl group, R2 and R3 are a gas and wherein A is selected from the group A3. Bel to A3. Be81. a compound of the formula la and a salt thereof, wherein R, 2 and R3 are hydrogen and wherein a is selected from the group A3. Bfl to A3. Bf81. A compound of the formula 1a and a salt thereof wherein R1 is a methyl group, R2 and R3 are a gas and wherein A is selected from the group A3. Bfl to A3. Bf81. 133661. Doc-83- 200917962 Table 290: Compounds of the formula la and salts thereof, wherein Ri is ethyl, sizing 2 and R3 are hydrogen and wherein A is selected from the group A3. Bfl to A3. Bf81. Table 291: Compounds of the formula la and salts thereof, wherein r1, R2 and R3 are hydrogen and wherein A is selected from the group A3. Bgl to A3. Bg81. Table 292: Compounds of the formula la and salts thereof, wherein R is methyl, and R3 is a gas wherein A is selected from the group A3. Bgl to A3. Bg81. Table 293: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 &amp; R3 is a gas and wherein A is selected from the group A3. Bgl to A3. Bg81. Table 294: Compounds of the formula la and salts thereof, wherein R1, Ruler 2 and Ruler 3 are hydrogen and wherein A is selected from the group A3. Bhl to A3. Bh81. Table 295: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, a sizing element 2 and an R3 group are chlorine and wherein the A group is selected from the group A3. Bhl to A3. Bh81. Table 296: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2 and R3 are gaseous and wherein A is selected from the group A3. Bhl to A3. Bh81. Table 297: Compounds of the formula la and salts thereof, wherein r1, R2 and R3 are hydrogen and wherein A is selected from the group A3. Bil to A3. Bi81. Table 298: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, a sizing element 2 and an R3 system gas, and wherein the A group is selected from the group A3. Bil to A3. Bi81. Table 299: Compounds of the formula la and salts thereof, wherein R1 is ethyl, r2 and R3 are gaseous and wherein A is selected from the group A3. Bil to A3. M81. Table 300: Compounds of the formula la and salts thereof, wherein R1, R2 and r3 are hydrogen and wherein A is selected from the group A3. Bkl to A3. Bk81. Table 3 0 1 : a compound of the formula la and a salt thereof, wherein R1 is a methyl group, r2 and R3 are a gas and wherein A is selected from the group A3. Bkl to A3. Bk81. 133661. Doc-84 - 200917962 Table 302: Compounds of the formula la and salts thereof, wherein R1 is ethyl, ... and Han 3 hydrogen, and wherein A is selected from the group A3. Bkl to A3. Bk81. Table 303. a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Bll to A3. Bl81. Table 304: Compounds of the formula la and salts thereof, wherein ... are methyl, R2 and R3 are hydrogen and wherein A is selected from the group A3. M1 to A3. Bl81. Table 305: Compounds of the formula la and salts thereof, wherein Ri is ethyl, and 3 is hydrogen and wherein A is selected from the group A3. M1 to A3. Bl81. Table 306: a compound of the formula la and a salt thereof, wherein the rule 2 and the rule 3 are hydrogen and wherein a is selected from the group A3. Bml to A3. Bm81. Table 307: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Bml to A3. Bm81. Table 308: Compounds of the formula la and salts thereof, wherein N is an ethyl group, "and a dentate 3 is hydrogen and wherein the A is selected from the group A3. Bml to A3. Bm81. Table 309: Compounds of the formula la and salts thereof, wherein Ri, R2 &amp; R3 are hydrogen and wherein a is selected from the group A3. Bnl to A3. Bn81. Table 310: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, R2 and R3 are hydrogen and wherein A is selected from the group A3 bnl to A3, bn81. Table 311: Compounds of the formula la and salts thereof, wherein Ri is ethyl, and 3 is hydrogen and wherein A is selected from the group A3. Bnl to A3. Bn81. Table 312: Compounds of the formula la and salts thereof wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Bol to A3. Bo81. TABLE 3 1 3 : Compounds of the formula la and salts thereof, wherein are methyl, R 2 and R 3 are gases and wherein A is selected from the group A 3 . Bol to A3. Bo81. 133661. Doc * 85 - 200917962 Table 314: Compounds of the formula la and salts thereof, wherein R and 3 are hydrogen and wherein A is selected from the group A3. Cal to A3. Ca81. Table 315: Compounds of the formula la and salts thereof, wherein R1 is methyl, and ampendix 3 is gas and wherein A is selected from the group A3. Cal to A3. Ca81. Table 316: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2&amp;R3 is a gas and wherein A is selected from the group A3. Cal to A3. Ca81. Table 317: Compounds of the formula la and salts thereof, wherein r1, R2 and R3 are hydrogen and wherein A is selected from the group A3. Cbl to A3. Cb81. Table 318: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, and R3 is a gas wherein A is selected from the group A3. Cbl to A3. Cb81. Table 319: Compounds of the formula la and salts thereof, wherein R1 is ethyl, sizing 2 and R3 are gaseous and wherein A is selected from the group A3. Cbl to A3. Cb81. Table 320: Compounds of the formula la and salts thereof, wherein r1, R2 and R3 are hydrogen and wherein A is selected from the group A3. Ccl to A3. Cc81. Table 321 : Compounds of the formula la and salts thereof, wherein Ri is methyl, R 2 and R 3 are gaseous and wherein A is selected from the group A3. Ccl to A3. Cc81. Table 322: Compounds of the formula la and their salts, of which! ^ is ethyl, and R3 is a gas and wherein A is selected from the group A3. Ccl to A3. Cc81. Table 323: Compounds of the formula la and salts thereof, wherein ri, 尺 2 and 尺3 are hydrogen and wherein a is selected from the group A3. Cdl to A3. Cd8 1. Table 324: Compounds of the formula la and salts thereof, wherein Ri is methyl, ft 2 and R3 are gaseous and wherein A is selected from the group A3. Cdl to A3. Cd81. Table 325: Compounds of the formula la and salts thereof wherein ri is ethyl, r2 and r3 are gases and wherein A is selected from the group A3. Cdl to A3. Cd81. 133661. Doc-86 - 200917962 Table 326: Compounds of the formula la and salts thereof, wherein Ri, R2 &amp; R3 are hydrogen and wherein a is selected from the group VIII 3^1 to VIII. 〇681. Table 327: Compounds of the formula la and salts thereof, wherein the ruthenium is a fluorenyl group, the sizing 2 and the sizing 3 are hydrogen and wherein the A is selected from the group A3. Cel to A3. Ce81. Table 328: Compounds of the formula la and salts thereof, wherein R is ethyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Cei to A3. Ce81. Table 329: Compounds of the formula la and salts thereof, wherein Ri, R2 &amp; R3 are hydrogen and wherein A is selected from the group A3. Cfl to A3. Cf81. Table 330: Compounds of the formula la and salts thereof, wherein Ri is methyl, and 3 is hydrogen and wherein A is selected from the group A3. Cfl to A3. Cf81. Table 331: Compounds of the formula la and salts thereof, wherein Ri is ethyl, and 3 is hydrogen and wherein A is selected from the group A3. Cfl to A3. Cf81. Table 332: Compounds of the formula la and salts thereof, wherein Ri, Ruler 2 and Rule 3 are hydrogen and wherein A is selected from the group A3. Cgl to A3. Cg8 1. Table 333: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, the ft 2 and the ft 3 are hydrogen and wherein the A is selected from the group A3 cgl to A3. Cg81. Table 334: Compounds of the formula la and salts thereof, wherein Ri is ethyl, sizing 2 and sizing 3 are hydrogen and wherein A is selected from the group A3. Cgl to A3. Cg81. Table 335: Compounds of the formula la and salts thereof, wherein r|, R2 and R3 are hydrogen and wherein A is selected from the group A3. Chl to A3. Ch81. Table 336: Compounds of the formula la and salts thereof, wherein R! is methyl, ft. 2 and amp. 3 are hydrogen and wherein A is selected from the group A3. Chi to A3. Ch81. Table 337: Compounds of the formula la and salts thereof, wherein Ri is ethyl' and the ampere 3 is hydrogen and wherein A is selected from the group A3. Chi to A3. Ch81. 133661. Doc-87· 200917962 Table 338: Compounds of the formula la and salts thereof, wherein R, R2 and R3 are hydrogen and wherein a is selected from the group A3. Cil to A3. Ci81. Table 339: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, ... and a Han 3 gas, and wherein the A group is selected from the group A3. Cil to A3. Ci81 〇 Table 340: a compound of the formula la and a salt thereof, wherein R is an ethyl group, and a genus 3 is hydrogen and wherein the A group is selected from the group A3. Cil to A3. Ci81. Table 341: Compounds of the formula la and salts thereof, wherein R!, R2 and R3 are hydrogen and wherein a is selected from the group A3. Ckl to A3, ck81. Table 342: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, ... and a Han 3 series hydrogen and wherein the A group is selected from the group A3. Ckl to A3. Ck81. Table 343: Compounds of the formula la and salts thereof, wherein R is ethyl, ... and Han 3 gas and wherein A is selected from the group A3. Ckl to A3. Ck81. Table 344: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Cll to A3. C181. Table 345: a compound of the formula la and a salt thereof wherein r1 is a fluorenyl group, R2 and R3 are a gas and wherein A is selected from the group A3. Cll to A3. C181. Table 346: a compound of the formula la and a salt thereof wherein Ri is an ethyl group, the rule 2 and R3 are hydrogen and wherein A is selected from the group A3. Cli to A3. C181. Table 347: Compounds of the formula ia and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Cml to A3. Cm81. Table 348: Compounds of the formula la and salts thereof, wherein R is methyl, and 2 and R3 are hydrogen and wherein A is selected from the group A3. Cml to A3. Cm81. Table 349: Compounds of the formula Ia and salts thereof, wherein Ri is ethyl, sizing 2 and R3 are hydrogen and wherein A is selected from the group A3. Cml to A3. Cm81 〇 133661. Doc-88- 200917962 Table 350: Compounds of the formula la and salts thereof, wherein R1, R2&amp; R3 are hydrogen and wherein a is selected from the group A3. Cnl to A3. Cn81. Table 351: Compounds of the formula la and salts thereof, wherein R1 is methyl, ... and Han 3 is hydrogen and wherein A is selected from the group A3. Cnl to A3. Cn81. Table 352: Compounds of the formula la and salts thereof, wherein R1 is ethyl, "and ... is hydrogen and wherein A is selected from the group A3 cnl to A3. Cn81. Table 353: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A3_co1 to A3. Co8 1. Table 354: Compounds of the formula la and salts thereof, wherein R1 is fluorenyl, R2 and R3 are hydrogen and wherein A is selected from the group A3. Col to A3. Co81 〇 Table 355: a compound of the formula la and a salt thereof, wherein Ri' R2 and R3 are hydrogen and wherein A is selected from the group A3. Dal to A3. Da81. Table 3 56: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 and R3 are hydrogen and wherein A is selected from the group A3. Dal to A3. Da81. Table 3 57: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Dal to A3. Da81. Table 358: Compounds of the formula la and salts thereof, wherein R1, Ruler 2 and R3 are hydrogen and wherein A is selected from the group A3. Dbl to A3. Db81. Table 3 59: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, R2 and R3 are a gas and wherein A is selected from the group A3. Dbl to A3. Db81. Table 360: Compounds of the formula la and salts thereof, wherein R1 is ethyl, sizing 2 and R3 are gaseous and wherein A is selected from the group A3. Dbl to A3. Db81. Table 361: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A3. Dc 1 to A3. Dc8 1. 133661. Doc •89· 200917962 Table 362: Compounds of the formula la and salts thereof, wherein Ri is methyl, R 2 and R 3 are hydrogen and wherein A is selected from the group A3. Del to A3. Dc81. Table 363: Compounds of the formula la and salts thereof, wherein R! is ethyl, R2&amp;R3 is hydrogen and wherein A is selected from the group A3. Dcl to A3. Dc81. Table 364: Compounds of the formula la and salts thereof, wherein Ri, Ruler 2 and R3 are hydrogen and wherein A is selected from the group A3. Ddl to A3. Dd81. Table 365: Compounds of the formula la and salts thereof wherein Ri is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Ddl to A3. Dd81. Table 366: a compound of the formula la and a salt thereof, wherein R! is an ethyl group, and a calilem 3 is hydrogen and wherein A is selected from the group A3. Ddl to A3. Dd81. Table 367: Compounds of the formula la and salts thereof, wherein R2&amp;R3 is hydrogen and wherein A is selected from the group A3. Del to A3. De81. Table 3: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Del to A3. De81. Table 69: Compounds of the formula la and salts thereof, wherein R! is an ethyl group, and a genus 3 is a gas and wherein the A group is selected from the group A3. Del to A3. De81. Table 3 70: a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A3. Dfl to A3. Df81. Table 371: Compounds of the formula la and salts thereof, wherein R1 is methyl, sizing 2 and sizing 3 and wherein A is selected from the group A3. Dfl to A3. Df81. Table 3 72: a compound of the formula la and a salt thereof, wherein R1 is an ethyl group, a ruthenium 2 and a R3 system gas, and wherein the A group is selected from the group A3. Dfl to A3. Df81. Table 373: Compounds of the formula la and salts thereof wherein R1, R2 and R3 are hydrogen and wherein a is selected from the group A3. Dgl to A3. Dg81. 133661. Doc-90- 200917962 Table 3 74: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Dgl to A3. Dg81. Table 375: Compounds of the formula la and salts thereof, wherein R1 is ethyl, "and Han 3 hydrogen" and wherein A is selected from the group A3. Dgl to A3. Dg81. Table 376: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Dhl to A3. Dh81. Table 3 77: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Dhl to A3. Dh81. Table 378: Compounds of the formula la and salts thereof, wherein Ri is ethyl, and 3 is chlorine and wherein A is selected from the group A3. Dhl to A3. Dh81. Table 379: Compounds of the formula la and salts thereof, wherein Ri, R2 &amp; R3 are hydrogen and wherein a is selected from the group A3. Dil to A3. Di81. Table 3 80: Compounds of the formula la and salts thereof, wherein r/ is methyl, R2&amp; R3 is hydrogen and wherein A is selected from the group A3. Dil to A3. Di81. Table 381: Compounds of the formula la and salts thereof, wherein Ri is ethyl and 3 is gas and wherein A is selected from the group A3. Dil to A3. Di81. Table 382: Compounds of the formula la and salts thereof, wherein r1, R2&amp; R3 are hydrogen and wherein A is selected from the group A3. Dkl to A3. Dk81. Table 383: Compounds of the formula la and salts thereof, wherein rJ is a fluorenyl group, R2&amp; R3 is a chloro group and wherein A is selected from the group A3. Dkl to A3. Dk81. Table 3 84: Compounds of the formula la and salts thereof, wherein are ethyl, sizing 2 and R3, and wherein A is selected from the group A3. Dk 1 to A3. Dk8 1. Table 385: Compounds of the formula la and salts thereof wherein R1, Rule 2 and R3 are hydrogen and wherein A is selected from the group A3. Dll to A3. Dl81. 133661. Doc-91 - 200917962 Table 3 86: Compounds of the formula la and salts thereof, wherein ... is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Dll to A3. Dl81. Table 387: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2&amp;R3 is a gas and wherein A is selected from the group A3. Dll to A3, dl81. Table 388: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Dml to A3. Dm8 1. Table 389: Compounds of the formula la and their salts, of which! ^ is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Dm 1 to A3. Dm81. Table 390: a compound of the formula la and a salt thereof, wherein ... is an ethyl group, a ft 2 and a genus 3 hydrogen, and wherein the A is selected from the group A3. Dml to A3. Dm81. Table 391: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Dnl to A3. Dn81. Table 392: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3 dnl to A3. Dn81. Table 393: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 &amp; R3 is nitrogen and wherein A is selected from the group A3. Dnl to A3. Dn81. Table 394: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Dol to A3. Do81. Table 395: Compounds of the formula la and salts thereof, wherein are: fluorenyl, ... and Han 3 hydrogen and wherein the A is selected from the group A3. Dol to A3. Do81. Table 396: Compounds of the formula la and salts thereof, wherein Ri, R2AR3 are hydrogen and wherein a is selected from the group A3, eal to A3. Ea81. Table 397. Compounds of the formula la and salts thereof, wherein r1 is methyl, r2 and r3 are hydrogen and wherein A is selected from the group A3. Eal to A3. Ea81. 133661. Doc-92- 200917962 Table 3 98: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Eal to A3. Ea81. Table 399: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Ebl to A3. Eb81. Table 400: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, R2&R3 is hydrogen and wherein A is selected from the group A3. Ebl to A3. Eb81. Table 401: Compounds of the formula la and salts thereof, wherein Ri is an ethyl group, and the ampere 3 is hydrogen and wherein the A group is selected from the group A3. Ebl to A3. Eb81. Table 402: Compounds of the formula la and salts thereof, wherein Ri, R2 & R3 are hydrogen and wherein a is selected from the group A3. Ecl to A3. Ec81. Table 403: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, the sizing elements 2 and 3 are hydrogen and wherein the A group is selected from the group A3. Eel to A3. Ec81. Table 404: Compounds of the formula la and salts thereof wherein Ri is ethyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Eel to A3. Ec81. Table 405: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein a is selected from the group A3. Edl to A3. Ed81. Table 406: Compounds of the formula la and salts thereof, wherein Ri is methyl, R2 and R3 are gaseous and wherein A is selected from the group A3. Edl to A3. Ed81. Table 407: Compounds of the formula la and salts thereof wherein Ri is ethyl, R2 & R3 is a gas and wherein A is selected from the group A3. Edl to A3. Ed81. Table 408: Compounds of the formula la and salts thereof, wherein ri, R2 &amp; R3 are hydrogen and wherein A is selected from the group VIII. 661 to 8 3. 6681. Table 409: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, R2 and R3 are a gas and wherein A is selected from the group A3. Eel to A3. Ee81. 133661. Doc-93- 200917962 Table 410: Table 411: Table 412: Table 413: Table 414: Table 415: Table 416: Table 417: Table 418: Table 419: Table 420: Table 421: Compounds of the formula la and their salts, wherein Ri Is an ethyl group, R2 and R3 are hydrogen and wherein A is selected from the group A3. Eel to A3. Ee81. a compound of the formula la and a salt thereof, wherein Ri, the ruler 2 and the rule 3 are hydrogen and wherein a is selected from the group A3. Efl to A3. Ef8 1. a compound of the formula la and a salt thereof, wherein Ri is a fluorenyl group, and a sulphate 3 is a gas and wherein the A group is selected from the group A3. Efl to A3. Ef81. a compound of the formula la and a salt thereof, wherein Ri is an ethyl group, R2&amp;R3 is a gas and wherein the A is far from the group A3. Efl to A3. Ef81. a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Egl to A3. Eg81. a compound of the formula la and a salt thereof, wherein R is a methyl group, a sizing rule 2 and a sizing gas, and wherein the A is selected from the group A3. Egl to A3. Eg81. a compound of the formula la and a salt thereof, wherein Ri is an ethyl group, and a Han 3 hydrogen group and wherein the A group is selected from the group A3. Egl to A3. Eg81. a compound of the formula la and a salt thereof, wherein R1, R2&amp; R3 are hydrogen and wherein a is selected from the group A3. Ehl to A3. Eh81. a compound of the formula la and a salt thereof, wherein Ri is a methyl group, R2 and R3 are hydrogen and wherein A is selected from the group A3 ehl to A3. Eh81. a compound of the formula la and a salt thereof, wherein R1 is ethyl, ... and Han 3 hydrogen, and wherein A is selected from the group A3. Ehl to A3. Eh81. a compound of the formula la and a salt thereof, wherein Ri, ... and R3 are hydrogen and wherein a is selected from the group A3. Eil to A3. Ei81. a compound of the formula la and a salt thereof, wherein Ri is a fluorenyl group, the quaternary 2 and the R 3 are hydrogen and wherein the A is selected from the group A3. Eil to A3. Ei81. 133661. Doc-94· 200917962 Table 422: Table 423: Table 424: Table 425: Table 426: Table 427: Table 428: Table 429: Table 430: Table 431: Table 432: Table 433: Compounds of the formula la and their salts, wherein R Is an ethyl group, R2 and R3 are hydrogen and wherein A is selected from the group A3. Eil to A3. Ei81. a compound of the formula la and a salt thereof, wherein R1, ... and 3 are hydrogen and wherein a is selected from the group A3. Ekl to A3. Ek81. a compound of the formula la and a salt thereof, wherein R1 is a methyl group, and the rule 2 and the rule 3 are hydrogen and wherein the A group is selected from the group A3. Ekl to A3. Ek81. a compound of the formula la and a salt thereof, wherein R1 is an ethyl group, the rule 2 and the rule 3 are hydrogen and wherein the A group is selected from the group A3. Ekl to A3. Ek81. a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group VIII. 611 to 8 3. 〇181. A compound of the formula la and a salt thereof, wherein R is a methyl group &quot; and a sulphate 3 is hydrogen and wherein the A is selected from the group A3. Ell to A3. El81. A compound of the formula la and a salt thereof wherein Ri is an ethyl group, R2 and R3 are hydrogen and wherein A is selected from the group A3. Ell to A3. El81. a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Eml to A3. Em8 1. a compound of the formula la and a salt thereof, wherein the methyl group, the rule 2 and the rule 3 are hydrogen and wherein the A group is selected from the group A3. Eml to A3. Em81. a compound of the formula la and a salt thereof, wherein Ri is ethyl, R2 &amp; R3 is hydrogen and wherein A is selected from the group A3. Ernl to A3. Em81. a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A3. Enl to A3. En81. And a salt thereof, wherein Ri is a fluorenyl group, R2 and r3 are hydrogen and wherein A is selected from the group A3. Enl to A3. En81. 133661. Doc-95- 200917962 Table 434: Compounds of the formula la and salts thereof, wherein R1 is ethyl and R3 is gaseous and wherein A is selected from the group A3. Enl to A3. En81. Table 435: Compounds of the formula la and salts thereof, wherein r1, R2 and R3 are hydrogen and wherein a is selected from the group A3. Eol to A3. Eo81. Table 436: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, r2 and R3 are a gas and wherein the A group is selected from the group A3. Eol to A3. Eo81. Table 437: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A3. Fal to A3. Fa81. Table 438: Compounds of the formula la and salts thereof, wherein R1 is methyl, ft 2 and amp 3 are nitrogen and wherein A is selected from the group A3. Fal to A3. Fa81. Table 439: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2 and R3 are nitrogen and wherein A is selected from the group A3. Fal to A3. Fa81. Table 440: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A3. Fbl to A3. Fb81. Table 44: Compounds of the formula la and salts thereof, wherein R1 is methyl, R2 and r3 are nitrogen and wherein A is selected from the group A3. Fbl to A3. Fb81. Table 442: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2 and r3 are chlorine and wherein A is selected from the group A3. Fbl to A3. Fb81. Table 443: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein A is selected from the group A3. Fcl to A3. Fc81. Table 444: Compounds of the formula la and salts thereof, wherein R1 is a fluorenyl group, R2 and r3 are a gas and wherein A is selected from the group A3. Fcl to A3. Fc81. Table 445: Compounds of the formula la and salts thereof, wherein R1 is ethyl, R2&amp;R3 is a gas and wherein A is selected from the group A3. Fcl to A3. Fc81. 133661. Doc-96- 200917962 Table 446: Compounds of the formula la and salts thereof, wherein Ri, R2 &amp; R3 are hydrogen and wherein a is selected from the group A3. Fdl to A3. Fd81. Table 447: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, a quaternary 2 and a &lt;3 gas and wherein the A is selected from the group A3. Fdl to A3. Fd81. Table 448: Compounds of the formula la and salts thereof, wherein Ri is ethyl, Han 2 and is hydrogen and wherein A is selected from the group A3. Fdl to A3. Fd81. Table 449: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Fel to A3. Fe81. Table 450: Compounds of the formula la and salts thereof, wherein Ri is methyl, and 3 is a gas and wherein A is selected from the group A3. Fel to A3. Fe81. Table 451: Compounds of the formula la and salts thereof, wherein Ri is ethyl, sizing 2 and sizing 3 are hydrogen and wherein A is selected from the group A3. Fel to A3. Fe81. Table 452: Compounds of the formula la and salts thereof, wherein the rule 2 and the rule 3 are hydrogen and wherein the A is selected from the group A3.  Ff 1 to A3.  Ff8 1. Table 453: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, "and a dentate 3 is hydrogen and wherein the A is selected from the group A3. Ffl to A3. Ff81. Table 454: Compounds of the formula la and salts thereof, wherein Ri is ethyl and sulphate is hydrogen and wherein A is selected from the group A3. Ffl to A3. Ff81. Table 455: Compounds of the formula la and salts thereof, wherein Ri, R2 and R3 are hydrogen and wherein A is selected from the group A3. Fgl to A3. Fg81. Table 456: Compounds of the formula la and salts thereof, wherein R is methyl, R2 and R3 are hydrogen and wherein A is selected from the group A3. Fgl to A3. Fg81. Table 457: Compounds of the formula la and salts thereof, wherein Ri is ethyl, R2 and R3 are hydrogen and wherein A is selected from the group A3. Fgl to A3. Fg81. 133661. Doc-97- 200917962 Table 458: Table 459: Table 460: Table 461: Table 462: Table 463: Table 464: Table 465: Table 466: Table 467: Table 468: Table 469: Compounds of the formula la and their salts, wherein Ri , R 2 and R 3 are hydrogen and wherein a is selected from the group A3. Fhl to A3. Fh81. a compound of the formula la and a salt thereof, wherein Ri is a fluorenyl group, and a sulphate 3 system gas and wherein the A group is selected from the group A3. Fhl to A3. Fh81. a compound of the formula la and a salt thereof, wherein Ri is an ethyl group, and a genus 3 is a gas and wherein the A group is selected from the group A3. Fhl to A3. Fh81. a compound of the formula la and a salt thereof, wherein Ri, ... and 3 are hydrogen and wherein a is selected from the group Α 3. Π1 to Α3. Π81. a compound of the formula la and a salt thereof, wherein Ri is a methyl group, "and a sulphide 3 gas and wherein the A is selected from the group A3. Fi 1 to A3. Π81. a compound of the formula la and a salt thereof, wherein R is an ethyl group, "and a sulphate 3 gas and wherein the A group is selected from the group A3. Fil to A3. Fi81. a compound of the formula la and a salt thereof, wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Fkl to A3. Fk81. a compound of the formula la and a salt thereof, wherein R] is a fluorenyl group, a trans 2 and a trans 3 system gas, and wherein the A group is selected from the group A3. Fkl to A3. Fk81. a compound of the formula la and a salt thereof, wherein is an ethyl group, R2 and R3 are a gas and wherein the A group is selected from the group A3. Fkl to A3. Fk81. a compound of the formula la and a salt thereof, wherein Ri, ... and trans 3 are hydrogen and wherein a is selected from the group A3. Fll to Α3. Π 8 1. a compound of the formula la and a salt thereof, wherein is a fluorenyl group, R2&amp;R3 is a gas and wherein A is selected from the group A3. Fll to A3. Fl81. a compound of the formula la and a salt thereof, wherein Ri is an ethyl group, a ruthenium 2 and a R3 system gas, and wherein the A group is selected from the group A3. Fll to A3. Fl81. 133661. Doc-98- 200917962 Table 470: Compounds of the formula la and salts thereof wherein Ri, R2 and R3 are hydrogen and wherein a is selected from the group A3. Fml to A3. Fm81. Table 471: Compounds of the formula la and salts thereof, wherein Ri is a fluorenyl group, and a Han 3 gas and wherein the A group is selected from the group A3. Fml to A3. Fm81. Table 472: a compound of the formula la and a salt thereof wherein Ri is an ethyl group, and a calilem 3 is a gas and wherein the A group is selected from the group A3. Fml to A3. Fm81. Table 473: Compounds of the formula la and salts thereof, wherein R!, Rule 2 and R3 are hydrogen and wherein a is selected from the group A3. Fnl to A3. Fn81. f Table 474: Compounds of the formula la and salts thereof, wherein Ri is methyl, ft 2 and Han 3 gas and wherein A is selected from the group A3. Fnl to A3. Fn81. Table 475: Compounds of the formula la and salts thereof, wherein Ri is ethyl, "and Han 3 gas and wherein A is selected from the group A3. Fnl to A3. Fn81. Table 476: Compounds of the formula la and salts thereof, wherein R1, R2 and R3 are hydrogen and wherein a is selected from the group A3. F〇l to A3. Fo81. Table 477 . a compound of the formula la and a salt thereof, wherein the Ri is a fluorenyl group, the quaternary 2 and the r3 are hydrogen and wherein the A is selected from the group A3. Fol to A3. F〇81. The compound of formula I or II can be prepared by standard methods of organic chemistry, for example by the methods described below or in the working examples: wherein Si is a ruthenium and X3 is a lone pair of Si compounds according to, for example, a scheme The method illustrated in 1 is activated by activation. It is prepared by reacting (4) biopterin with the 3_aminopyridine compound m (see, for example, Houben_we Juice &quot;Methoden Chemistry] der organ.  Chemie&quot; [Methods 〇f 〇rganic Georg-Thieme-Verlag, Stuttgart, New York Activated α vs. Sputum Derivatives Π 1985, Vol. E5, pp. 941_1〇 45 133661. Doc •99- 200917962 is, for example, a complex, activated brewing, acid needle, 4 nitride, such as chloride, fluoride, bromide, p-nitrophenyl ester, pentafluorophenyl ester 'ice hydroxy amber Amine, hydroxybenzotriazolyl ester. In the scheme, the bases: A R R and R have the above meanings and in particular have the preferred meanings, and X is a suitable leaving group such as _ 素, %, ω phenoxy and the like. &lt; Option 1: A, ΟΙ)

(III)(III)

其中X為〇且χ3為孤雷+管 + τ 冤子對之式1活性化合物亦可(例如) 根據方案2藉由在偶合劑存在下使吼唑羧酸胺美吼 咬化合物m反應來製備。在方案2中,基^、^及 R3具有上述含義且尤其具有所述較佳之含義。 方案2 :Wherein X is hydrazine and χ3 is a lone thunder + tube + τ 冤 对 pair of the active compound of formula 1 can also be prepared, for example, according to Scheme 2 by reacting a carbazole carboxylic acid amine quinone bite compound m in the presence of a coupling agent. . In Scheme 2, the radicals, ^ and R3 have the above meanings and in particular have the preferred meanings. Scenario 2 :

Ο R A人 OH + Η、Ο R A person OH + Η,

(IV) (Hi) 適宜偶合劑係(例如): 基於碳化二亞胺之偶合劑,例如N,N,-二環己基_碳化 -亞即X. Sheehan,G.P. Hess,J Am. Chem. s〇c. 133661.doc •100- 200917962 1955,77, 1067]、N-(3-二甲基胺基丙基)-Ν·-乙基碳化 —亞胺, -與碳酸酯形成混合酸酐之偶合劑,例如2-乙氧基-1-乙 氧基羰基-1,2-二氫喹啉[B. Belleau,G. Malek, J. Amer. Chem. Soc. 1968, 90,1651]、2-異丁氧基-1-異 丁氧基羰基-1,2-二氫喹啉[Y. Kiso,H. Yajima,J. Chem. Soc.,Chem. Commun. 1972,942]; -基於鱗鹽之偶合劑,例如(苯并三唑-1-基氧)三(二甲 基胺基)六氟磷酸鱗[B. Castro,J.R. Domoy,G. Evin, C. Selve,Tetrahedron Lett. 1975,14,1219]、(苯并三 唑-1-基-氧)三吡咯啶并六氟磷酸鱗[j· Coste等人, Tetrahedron Lett. 1990, 31, 205]; - 基於錁鹽或具有胍鏽N -氧化物結構之偶合劑,例如 Ν,Ν,Ν',Ν'-四曱基-0-(1 H-苯并三唑-1-基)六氟磷酸錁 [R. Knorr, A. Trzeciak, W. Bannwarth, D. Gillessen, Tetrahedron Lett. 1989,30,1927]、N,N,N',N·-四甲基_ 〇-(苯并三唑-1-基)四氟硼酸錁、(苯并三唑基氧)二 六氫°比啶并六氟磷酸碳鏽[S. Chen,J. xu,Tetrahedn)n Lett. 1992, 33, 647]; - 形成醯氣之偶合劑,例如雙-(2·氧-噁唑咬基)次鱗醯 氯[J· Diago-Mesequer, Synthesis 1980, 547] ° 其中X為〇、X3為孤電子對且R1不為氫之化合物I亦可藉 由在鹼存在下使用適宜烷基化劑使醯胺1(其中R1係氣且其 可根據方案1或2來獲得)烷基化來製備。 133661.doc -101 - 200917962(IV) (Hi) Suitable coupling agents (for example): carbodiimide-based coupling agents, such as N, N,-dicyclohexyl carbyl--- ie X. Sheehan, GP Hess, J Am. Chem. s 〇c. 133661.doc •100- 200917962 1955,77, 1067], N-(3-dimethylaminopropyl)-anthracene-ethylcarbide-imine, - forming a mixed anhydride with carbonate Mixtures, for example 2-ethoxy-1-ethoxycarbonyl-1,2-dihydroquinoline [B. Belleau, G. Malek, J. Amer. Chem. Soc. 1968, 90, 1651], 2- Isobutoxy-1-isobutoxycarbonyl-1,2-dihydroquinoline [Y. Kiso, H. Yajima, J. Chem. Soc., Chem. Commun. 1972, 942]; a coupling agent such as (benzotriazol-1-yloxy)tris(dimethylamino)hexafluorophosphate scale [B. Castro, JR Domoy, G. Evin, C. Selve, Tetrahedron Lett. 1975, 14 , 1219], (benzotriazol-1-yl-oxy)tripyrrolidinium hexafluorophosphate scale [j. Coste et al, Tetrahedron Lett. 1990, 31, 205]; - based on strontium salts or with rust N - a coupling agent for an oxide structure, such as ruthenium, osmium, iridium, Ν'-tetradecyl-0-(1H-benzotriazol-1-yl)hexafluorophosphate [R. Knorr, A. Trzeciak, W. Bannwarth, D. Gillessen, Tetrahedron Lett. 1989, 30, 1927], N, N, N', N·-tetramethyl 〇 (-(benzotriazole-1 -based) bismuth tetrafluoroborate, (benzotriazolyloxy) dihexahydropyrene hexafluorohexafluorophosphate [S. Chen, J. xu, Tetrahedn) n Lett. 1992, 33, 647]; Forming a coupling agent for helium, such as bis-(2. oxo-oxazole bite) squamous chlorine [J. Diago-Mesequer, Synthesis 1980, 547] ° where X is 〇, X3 is a lone pair and R1 is not Compound I which is hydrogen can also be prepared by alkylation of indoleamine 1 (wherein R1 is gas and which can be obtained according to Scheme 1 or 2) using a suitable alkylating agent in the presence of a base. 133661.doc -101 - 200917962

吡唑羧酸iv及其經活化衍峰榀ττ、,„ ^ Α 丁生物11 u及3 -胺基σ比咬化合物 III係業内已知或自市場上購媒弋—Ρ V Λ #嗎仔或可藉由文獻中所述之方法 來製備。 其中X1不為氧之式I化合物可藉由標準方法自化合物㈣ 製備: 其中X1為S之式他合物可(例如)根據M· Jesberger等人, Synthesis 2003, 1929中所述方法藉由使化合物13與2,4-雙 (4-甲氧基苯基)-1,3,2,4-二硫二磷烷(dithiadiph〇sphetane) 2,4-二硫化物或五硫化碟反應來製備。 其中X1為ΝΙ^之式了化合物可(例如)根據v⑴⑽以…等 人,Pharmaceutical Chemistry Journai 2〇〇5,39(10) ’ 533_Pyrazole carboxylic acid iv and its activated derivative peaks 榀ττ, „ ^ 生物 生物 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 11 Alternatively, it can be prepared by the methods described in the literature. The compound of formula I wherein X1 is not oxygen can be prepared from compound (iv) by standard methods: wherein X1 is a compound of S can be, for example, according to M. Jesberger The method described in Synthesis 2003, 1929 by using compound 13 with 2,4-bis(4-methoxyphenyl)-1,3,2,4-dithiodiphosphane (dithiadiph〇sphetane) The 2,4-disulfide or pentasulfide dish is prepared by reacting. The compound wherein X1 is ΝΙ^ can be, for example, according to v(1)(10), etc., Pharmaceutical Chemistry Journai 2〇〇5, 39(10) ' 533_

536中所述方法藉由以下方式來製備:使化合物1&amp;與2,4-雙 (4-曱氧基苯基)-1,3,2,4-二硫二磷烷_2,4_二硫化物反應以 獲得對應硫代醯胺(化合物I,其中χι係s),之後使其與適 宜胺反應。 其中X2=SR2a之式II化合物可根據v Glushk〇v等人,The method described in 536 is prepared by reacting Compound 1 &amp; with 2,4-bis(4-decyloxyphenyl)-1,3,2,4-dithiodiphosphane-2,4_ The disulfide reaction is carried out to obtain the corresponding thioguanamine (Compound I, wherein χι is s), which is then reacted with a suitable amine. The compound of formula II wherein X2=SR2a can be used according to v Glushk〇v et al.

Pharmaceutical Chemistry J〇urnal 2005, 39(10),533-536 中 所述之方法藉由使對應硫代醯胺(化合物I,其中χι係s)與 烧基化劑反應以使其烧基化來製備。以類似方式可獲得其 中 X2 為 OR2a 或 NR2bR2ci 化合物 I。其中 x2=s〇R2a 或 s〇2R2a 133661.doc •102· 200917962 之式II化合物可藉由氧化其中X2=SR2a夕几人 之化合物II來獲得。 其中X為〇之式I及11化合物可枢擔制很 J根據製備吡啶Ν-氧化物之 標準方法藉由氧化其中Χ3為孤電子對之化合物工來製備, 例如藉由 c. B〇tteghi 等人,Journal 〇f 〇rg繼metaiiicThe method described in Pharmaceutical Chemistry J〇urnal 2005, 39(10), 533-536 is carried out by reacting a corresponding thioguanamine (Compound I, wherein χι s) with an alkylating agent to cause it to be alkylated. preparation. In a similar manner, X2 is OR2a or NR2bR2ci Compound I. Wherein compound of formula II wherein x2 = s 〇 R2a or s 〇 2R2a 133661.doc • 102· 200917962 can be obtained by oxidizing compound II wherein X2 = SR2a. The compounds of formulas I and 11 wherein X is ruthenium can be prepared by a standard method for preparing pyridinium-oxide by oxidizing a compound in which ruthenium 3 is a lone pair, for example, by c. B〇tteghi et al. Person, Journal 〇f 〇rg following metaiiic

ChemiStry 1989, 3 70, 1 7-3 i中所述之方法來製備 通常,式1或Π化合物可藉由上述方法來製備。若不心 由上述路徑製備各個化合物,則其可藉由其他化合物則 2何生或蜡由對所述合成路徑之習知改變來製備。舉例而 吕,在各種情況下’某些化合物I哎 加 及11有利地可藉由酯水 解、醯胺化、S旨化、_裂解、稀化 遏原、乳化及類似方 式自其他化合物I或II來製備。 可以習知方式處理反應混合物,例如藉由與水混合、分 離各相及(若適宜)藉由層析(例如在氧化紹或石夕夥上)純化 粗產物來處理。可以無色或淡栋色黏稠油形式獲得某些中 間體及終產物’其在低壓及適度汽 迥度同/皿下游離於揮發性組份 〆自揮發性組伤純化。若以固體形式傅彳θ &amp; π ^ 短仏式獲侍中間體及終產 物,則可藉由再結晶或研磨將其純化。 由於通式咖化合物具㈣㈣活性,其可用於控制無 脊椎害蟲。 因此,本發明亦提供控制無脊椎害蟲之方法,該方法包 含用殺蟲有效量的上文所定義之式⑴或(π)化合物或其鹽 或Ν-氧化物或組合物處理宝 口蛾其食物供應、其棲息地或 其繁殖地、或其中生長哎可哇具 生長害蟲之栽培植物、植物 殖材料(例如種子)、土墣 ,,^ ’、 壤、&amp;域、材料或環境、或欲防止 I33661.doc 200917962 又到害蟲侵襲或侵擾之材料、栽培植物、植物繁殖材料 (例如種子)、土壤、表面或空間。 較佳地,本發明方法用於保護植物繁殖材料(例如種子) 及自其生長之植物免受無脊椎害蟲侵襲或侵擾,且包含用 杀又**有效里的上文所定義之式⑴或(I]t)化合物或其農業上 可,受之鹽或N-氧化物或用殺蟲有效量之上下文;所定義 之農業組合物處理植物繁殖材料(例如種子)。本發明方法 亚不限於對已根據本發明處理之”基質”(植物、植物繁殖材 料、土壤材料等)的保護,且由此對自經處理植物繁殖材 料(例如種子)生長之植物亦具有預防性效應(例如與經處理 植物繁殖材料-致的保護),纟中該植物自身係未經處 沈本么明而5,&amp;脊椎害蟲&quot;較佳係選自節肢動物及線 蟲’更佳係選自有害昆蟲、蜘蛛及線蟲,1甚至更佳係選 自昆蟲、蟎蟲及線蟲。 V. b本U進纟提供用於抵抗該等無脊椎害蟲之農 ’其包含殺蟲作用有效量之至少-種通式即化 合物或至少_種其農業上可用之鹽絲_氧化物、及至少一 接受之液體及/或固體惰性載劑、及(若需要) 至少一種表面活性劑。 根據本發明,此-組合物可含有單—活性式即化合物 或”皿或N氧化物 &lt; 右干種活性化合物!或η或其鹽之混 口物本心明組合物可包含單獨同分異構體或同分異構體 混合物以及單獨互變異構體或互變異構體混合物。 133661 .doc -104· 200917962 式I或II化合物及包含其之殺蟲組合物係控制節肢動物害 蟲及線蟲之有效試劑。受式I或II化合物控制之無脊椎宝蟲 包括(例如): 來自鱗翅目(鱗翅目之昆蟲,例如小地老 虎(dgro沿、黃地老虎(Jgro沿、棉葉波 紋葉蛾、黎豆夜蛾 gemwaia/b)、蘋實巢蛾co^/wge//a)、丫紋夜 蛾(Jwiograp/m gamma)、松尺獲(5wpa/w5· piWari.ws)、冷杉 粗卷蛾(Cacoecia mwr/nanci) ' 紅紋煙捲蛾(Capwa reiicw/ana)、冬尺蛾(C/zez·所βίοΜα 6rwm&lt;aia)、雲杉卷葉蛾 {Choristoneura fumiferana)、 西 方雲杉 卷葉蛾 {Choristoneura occidentalis)、 美;ί、州毒占蟲(Cirphis 、蘋果蠹蛾(C_y山、歐洲松毛蟲 [Dendrolimus pini)、瓜 ff 嗓{Diaphania nitidalis)、反良么 米堪[Diatraea 、埃及金剛鑕·(五以/似 insulana) &gt; 南美玉朱笼斑螺[Elasmopalpus lignosellus)、女 負細卷織(Eupoecilia ambiguella) '歐洲松梢小卷蛾 (Evetria bouliana)、粒詹地老底(Feltia subterranea)、大壤 缚{Galleria mellonella) ' 李小食心轰(Grapholitha funebrana)、梨小食心義[Grapholitha molesta)、棉铃备 [Heliothis armigera)、美洲煙葉織[Heliothis virescens)、 美洲構铃蟲^ (Heliothis zea)、象塔(Hellula undalis)、反镜 希伯利亞蛾(//76erm_a c?e/o/i’an_a)、美國白蛾(//_yp/zanir/c! cwnea)、蘋果巢蛾(if_yponc&gt;mewia 、蕃莊蠹蛾 133661.doc -105- 200917962 {Keiferia lycopersicella) ' {Lambdina fiscellaria) ' 甜菜夜蛾exigua)、咖啡點潛蛾 coffeella)、旋故潛案蛾^ {Leucoptera 、蘋細蛾 {Lithocolletis 、葡萄漿果小卷蛾(Zobeha 6oircma)、黃綠條螟(Loxcmege siiciica/b)、舞毒蛾 {Lymantria dispar) ' it ^ ^ ^{Lymantria monacha) ' 窄翅 潛葉蛾(L_yo«e&quot;iJ! clerkellcT)、天幕% 备 QMalacosoma newwr/fl)、甘藍夜蛾(Mawairo; 、黃杉毒蛾 psewiioiswgaia)、歐洲玉米模(〇5/W«z_a wwW/flD)、 冬夜蛾 QPanolis flammea) 、銜氣[Pectinophora 又pie//a)、豆雜角夜蛾'圓黃掌舟蛾 {Phalera bucephala)、馬铃集成 1 織(Phthorimaea opercw/eZ/a)、橘細潛蛾cz7re//a)、大菜粉蛾 、苜卷綠夜蛾(Ρ/αί/ζ 少/7 ⑼ a 、小菜 蛾{Plutella xylostella)、大豆夜蛾(Pseudoplusia 、松梢卷葉蛾(/?/z_yaciom‘a /rwsirawa)、馬鈴著塊 1 味[Scrobipalpula absoluta)、參織{Sitotroga cerealella)、 葡萄長須卷葉蛾(Sparganoi/ib ρί//6η·α«α)、草地黏蟲 (Spodoptera frugiperda)、海灰翅夜蛾(《Spoc/opiem littoralis)、斜紋夜蛾(*S/7〇i/〇/&gt;iera /z'iwrcz)、松異周蛾 (J’haumatopoea pityocampa) ' 機綠卷葉峨(Tortrix viridana) '粉故夜蛾(Tyichoplusia «/·)及雲杉小卷葉蛾 {Zeiraphera canadensis) » 曱蟲(輔翅目(Coleoptera)),例如梨長吉丁(Agrilus -106- 133661.doc 200917962 sinuatus)、具條叩甲(Agriotes lineatus)、暗紋0P 甲 (Agriotes obscurus)、六月金龜(Amphimallus solstitialis)、 異形方胸材小蠹(Anisandrus dispar)、棉鈴象甲 (Anthonomus grandis)、蘋果花象曱(Anthonomus pomorum)、甜菜隱食甲(Atomaria linearis)、大松小蠹 (Blastophagus piniperda)、粗紋小蜂(Blit'ophaga undata)、 蠢豆象(Bruchus runmanus)、婉豆象(Bruchus pisorum)、 歐洲兵豆象(Bruchus lentis)、韻果卷葉象曱(Byetiscus betulae).、甜菜大龜甲(Cassida nebulosa)、豆葉曱 (Cerotoma trifurcata)、甘藍莢象曱(Ceuthorrhynchus assimilis)、油菜龜象曱(Ceuthorrhynchus napi)、甜菜莖跳 甲(Chaetoenema tibialis)、煙草金針蟲(Conoderus vespertinus)、天門冬葉甲(Crioceris asparagi)、長角葉甲 (Diabrotica longicornis)、十二星瓜葉曱(Diabrotica 12-punctata)、玉米根葉甲(Diabrotica virgifera)、墨西哥豆瓢 蟲(Epilachna varivestis)、煙草跳甲(Epitrix hirtipennis)、 棉籽灰象(Eutinobothrus brasiliensis)、松樹皮象(Hylobius abietis)、埃及苜蓿象曱(Hypera brunneipennis)、苜稽葉象 甲(Hypera postica)、雲杉八齒小蠹(Ips typographus)、具 條負泥蟲(Lema bilineata)、黑角負泥蟲(Lema melanopus)、馬铃薯甲蟲(Leptinotarsa decemlineata)、甜 菜金針蟲(Limonius californicus)、稻象甲(Lissorhoptrus oryzophilus)、蘆葦叩頭蟲(Melanotus communis)、油菜露 尾甲(Meligethes aeneus)、忽布鰓角金龜(Melolontha 133661.doc •107· 200917962 hippocastani)、歐洲總金龜(Melolontha melolontha)、稻負 泥蟲(Oulema oryzae)、葡萄黑耳缘象(Ortiorrhynchus sulcatus)、草莓根象甲(Otiorrhynchus ovatus)、辣根猿葉 曱(Phaedon cochleariae)、油菜藍跳曱(Phyllotreta chrysocephala)、金龜屬(Phyllophaga sp.)、庭園麗金龜 (Phyllopertha horticola)、大豆淡足跳甲(Phyllotreta nemorum)、黃曲條跳甲(Phyllotreta striolata)、曰本麗金龜 (Popillia japonica)、豌豆葉象甲(Sitona lineatus)及穀象 (Sitophilus granaria); 雙翅類昆蟲(雙翅目,例如埃及伊蚊 、刺擾伊蚊似)、墨西哥橘實蠅 (Anastrepha ludens)、微按故〈Anopheles maculipennis、、 地中海貫繩(Cerai/ϋ 、姐症金 1¾ bezziana) ' 螺旋金繩(C/zrpowya ;7〇wz'm_vora;c)、肉旋金题 (Chrysomya macellaria)、高 粱癭蚊[Contarinia sorghicolcT)、嗜人瘤織(Cordylobia anthropophaga)、丘帶 淡色庫蚊(Cw/ex 瓜實蠅(Dacwj cwcwrZn7ae)、油 橄欖實蠅(Dacw 〇/eae)、芸苔莢癭蚊 、黃腹廄繩(Fa㈣ζ_α cam'cw/arb)、大馬胃蠅 {Gasterophilusintestinalis、、^^i^、Glossinamorsitans、' 綠優爯纖(Haematobia irritans)、鞍癭徵故(Haplodiplosis e分wairh)、種輝| p/aiwro)、蚊皮繩 、美洲斑潛繩(Zz’r/omyza saii’vae)、非洲菊斑潛姆 (Liriomyza 的/o/H)、羊綠蠅(Lwcz‘&quot;a ⑽)、銅綠蠅 133661.doc •108- 200917962 (Lucilia cuprina) ' 綵先綠規(Luciiia sericata)、玉頸洛先 蠅黑森癭蚊(Μαγη·ο/α AWrwcior)、 家蠅(Mwca 办廄腐蠅(Mwscka wMw/a似)、羊 鼻蠅(Oairw·? ovk)、瑞典麥桿蠅y&gt;&quot;)、甜菜潛 葉蠅(Pegomya /zwoc少awz·)、蔥蠅a/7&quot;《wa)、甘蘭 種蠅(P/zorha ^aMZ’cae)、麥種蠅(p;2〇rHa coarciak)、櫻 桃實蠅(灿叹0/如··? ceran’)、蘋果實蠅(心叹〇/e山 pomonella) 、 ^ it (Tabanus bovinus) ' 沼澤大蚊(TipuZa oleracea):^ 歡 if\\ 大蚊[Tipula paludosa&quot;) ·, 薊馬(纓翅目(77〇^«opiera)),例如蘭花薊馬 (Dichromothrips corbetti)、煙萆褐範馬(Frankliniella /wsca)、苜蓿薊馬(FrimWm'e//a occWenia/b)、麥花薊馬 {Frankliniella tritici)、橡 f 範馬(Scirtothrips citrV)、稻蘇 馬(Γ/2η&gt;·5 or少zae)、棕櫚萷馬(77zrz&gt;s pa/m/)及棉薊馬 {Thrips tabaci); 膜翅類(膜翅目(Hymenoptera)),例如新疆菜葉蜂 (Athalia rosae)、熱帶切葉蟻(Atta cephalotes)、切葉蟻 (Atta sexdens)、德州切葉蟻(Atta texana)、李小葉蜂 (Hoplocampa minuta)、蘋實葉蜂(Hoplocampa testudinea)、廚蛾(Monomorium pharaonis)、火犧 (Solenopsis geminata)及夕卜弓I 紅火蟻(Solenopsis invicta); 異翅類(異翅目(Heteroptera)),例如喜綠蜡(Acrosternum hilare)、多毛長蜂(Blissus leucopterus)、煙草黑斑盲培 (Cyrtopeltis notatus)、棉紅缚(Dysdercus cingulatus)、中 133661.doc -109- 200917962 間培(Dysdercus intermedius)、麥扁盾蝽(Eurygaster integriceps)、棉褐蜂(Euschistus impictiventris)、葉足緣 蝽(Leptoglossus phyllopus)、美國牧草盲蝽(Lygus lineolaris)、牧草盲蜂(Lygus pratensis)、稻綠墙(Nezara viridula)、甜菜撿網蜂(Piesma quadrata)、小綿角色魯蝽 (Solubea insularis)及普迪特梯蝽(Thyanta perditor); 同翅類(同翅目(//omopiera)),例如紅豆草财 {Acyrthosiphon onobrychis)、落葉松球蚜(Jc/e/gei laricis)、甘篆场(Aphidula nasturtii)、蠢 场(Aphis /a6ae)、草莓根財、蘋果财、 棉财gowypH)、醋栗虫牙groww/arz’ae)、茶蔴 财(/ip/zz··? sc/meWerz·)、繚線菊财(/ίρ/π··? 、接骨 表财(Aphis sambuci)、规瓦輯(Acyrthosiphon pisum)、% 溝 無網攝(Aulacorthum ·5〇/α«〇 、銀葉粉乱(方emb/a 、煙粉虱(Bemisia tabaci)、薊短尾財 (Brachycaudus cardui) &gt; 李短尾蚜 /2e/k/2r少d)、桃黑短尾蚜s pem'cae)、普魯内 考拉舌尾蚜、甘藍蚜 △ raw/cae)、角釘毛財(Caphop/zorws /zorm·)、棉花方翅網蜂 (Cerosipha gossypii)、萆莓毛 f 蚜(chaetosiphon 、命蘼隱瘤額財(Cryp/om少r/Ws)、高加索椎 球财(Drey/wha nordmannianae) ' 雲杉椎球財(Drey/MWa 、萊德考拉圓尾財ra&lt;:/z’c〇/a)、擬塘鶴财 (Dysaulacorthum psewdosolani)、鳋粉紅劣蚜(Dysaphis 133661.doc -110- 200917962 ⑽)、梨西圓尾蚜pyW)、蠶豆葉蟬 (Empoasca fabae)、梅大 I 场(Hyalopterus pruni)、茶藤告 菜财(i/xperomj/zws lactu-cae)、參長 f 蜗(Macrosiphum avewae)、大戟長管財(Macrosz’p/zwm ewp/zorb/ae)、薔薇長 管財(Macrohp/^ow rosae)、蠶豆修尾财(Megowra Wc/ae)、 帕洛瑞斯色財(Me/awap/n’s 、薔薇麥財 {Met opol op hi um dirhodum)、^ {Myzodes persicae) ' 冬 蔥瘤額蚜(Myzws c^ca/oWcw)、櫻桃黑瘤額蚜(似⑽ cerah)、桃蚜(M_yzWly perhC(3e)、核黃瘤額蚜(从少之心 var/aw)、蒿苣蚜(iVa&gt;so«ov/a 、褐稻虱(w/a_ parvaia /wge似)、萬苣根趨綿财6wriyar?‘Wi5)、蔗 飛虱(Perh«以_e//a Mcc/mricWa)、蛇麻疣額蚜(P;/〇r0t/o« 办www/z’)、蘋木風(尸sy/Za Wa//)、梨木乳(尸π//α pirz·)、冬蔥 縊瘤蚜{Rhopalomyzus ascalonicus)、玉米縊管蚜 {Rhopalosiphum maidis、、粟缢管蚜(Rhopa丨osiphum /?ac^·)、郁李溢管蚜 insertum)、梨石占草财 (Sappaphis wa/a)、多貝紅紮圓尾财Wa/z·)、麥二 又蚜(Schizaphis grawkwm)、榆梨棉蚜(Sc/n.zc^ewra /⑽wg/wow)、麥長管蚜(&amp;·/〇&amp;·〇« 此)、白背飛虱 {Sogatella /wrcz/era)、溫室白粉虱(JWa/ewoc/w vaporar/orww)、橘二岔蚜(7\?;c〇/^era awr&lt;a«&quot;i·)及葡萄根瘤 场[Viteus vitifolii) ’, 白礒(等翅目(Isoptera)),例如歐洲木白犧(Calotermes flavicollis)、歐美散白蟻(Leucotermes flavipes)、黃胸散白 133661.doc -111 - 200917962 蟻(Reticulitermes flavipes)、南歐網紋白蟻(Reticuiitermes lucifugus)及納塔爾白蟻(Termes natalensis); 直翅類(直翅目(Ori/zop⑽α)),例如家蟋蟀(JdeM ί/owai/ca)、東方斐蝶(β/α&quot;α or/ewiaD)、德國小蝶 (Blattella germanica)、歡洲來後(Forficula auricularia)、 歐洲樓姑(GryHoiaipa gryn〇ta!pa)、飛虫皇(Loewsk wz’grofMWa)、雙帶蚱蜢(Me/a«op/WlS 赤腿蚱蜢 (Melanoplus femurrubrum)、墨西哥蛑蜢(Melanoplus 、遷徒虫卞猛(Me/a/iop/ws 、落石幾山 碑蜢(Melanoplus spretus)、m(Nomadacris septemfasciata)、 美洲大蠊(Perz&gt;/㈣ek ameWc㈣α)、美洲蚱 amehca«a)、帕雷格林納蚱蜢⑽)、 Stauronotus 所 及溫室蟋螽(rac/〇;cz^ asynamorus); 蛛形綱(Aflc/moz·心a) ’例如蜘蛛(蜱蟎目ycar/wa)),例 如軟蜱科(drgim·而e)、硬蜱科(/x〇i/wae)及蚧蟎科 (〜rC〇Jp&quot;·而e) ’例如美洲花蜱以—矽⑽卿ameWc⑽謂)、 熱帶花蜱(dm6/_yowma vaWegaiwm)、波斯隱喙蜱(^尽似 perWcws)、具環方頭蜱⑽⑽以似)、消色牛碑 (Boophilus decoloratus)、微+牛蜱iBoophilus micr〇plus、、 森林革蜱(Der則_s//varww)、長&quot;彖璃眼蜱(//%/⑽腦 、蓖子硬蜱(/ΧΟύ^ rycz·”⑽)、淺紅硬蜱(^^心^ rubicundus)、兔辦(_〇rnithodorus moubata) ' 异殘。象缉 (Oiohw meg⑴·《/)、雞皮刺蟎(Der廳町以⑽抑//i&gt;me)、羊 133661.doc -112- 200917962 疼端(Psoroptes ovis) ' 具尾 M 頭碑(Rkipicephalus 山'cw/aiws)、外翻扇頭蜱ever/以·)、疮 虫高(》Sarcopie5· ααά/β/)及癭蜗科(五 Hop/zyzWae spp.),例如蘋 刺癭蜗(yicw/ws ίΆ/π/7ίβ«ΰ?β/ζ·)、橘鏽蜗(P/z&gt;&gt;//oc;o/?iraia o/e/vora)及柑芽癭蜗(五riop/zyes s/ze/i/om·);樹線瞒科 (Γααο加w/dae sppj,例如仙客來細蜗(尸/z_yicmemwj pallidus)反多食附緣織(Polyphagotarsonemus latus) ·,偽葉 蟎科(7&gt;«Μφα^αίαβ spp.),例如紫僞葉蟎(BreWpa/pw p/zoem'cb);葉瞒科(7&gt;ira^yc/H'c/(3e 577/?·),例如朱砂·葉蜗 (reira^yc/zz^ cz’⑽Marz'wws)、神澤氏葉蟎 Α:ίϊπζανναζ·)、太平洋紅葉蟎(7^ίΓαπ&lt;^Μ·5 pacz/icws)、棉紅葉 蟎(reira«_yc/2ws ie/arks)及棉葉蟎wri/cae)、 蘋果全爪蟎w/w〇、橘全爪蟎似 cz’in’)及草地小爪蜗(ongo/^c^ws praiewb); 蚤目(Siphonatera) ’ 例如東方鼠蚤(Xenopsylla cheopsis)、 角葉蚤屬(Ceratophyllus spp.)。 組合物及式I或II化合物可用於控制線蟲,尤其植物寄生 性線蟲,例如根瘿線蟲(root knot nematode)、北方根結線 蟲(Meloidogyne hapla)、南方根瘤線蟲(Meloidogyne incognita)、爪哇根結線蟲(Meloidogyne javanica)、及其他 根結線蟲屬(Meloidogyne)物種; 包囊線蟲(cyst-forming nematode)、馬鈐薯黃金線蟲 (Globodera rostochiensis)及其他黃金線蟲(Globodera)物 種;燕麥胞囊線蟲(Het-erodera avenae)、大豆胞囊線蟲 133661.doc •113· 200917962 (Heterodera glycines)、甜菜胞囊線蟲(Heterodera schachtii)、草胞囊線蟲(Heterodera trifolii)、及其他胞囊 線蟲(Heterodera)物種;種癭線蟲(Seed gall nematode)、蛇 墊刃屬(Anguina)物種;莖葉線蟲(Stem and foliar nematode)、滑刀線蟲屬(Aphelenchoide)物種;螯針線蟲 (Sting nematode)、松樹刺線蟲(Belonolaimus longicaudatus)及其他針刺線蟲(Belonolaimus)物種;松樹 線蟲(Pine nematode)、松材線蟲(Bursaphelenchus xylophilus)及其他松材線蟲(Bursaphelenchus)物種;環形 線蟲(Ring nematode)、環線蟲屬(Criconema)物種、小環線 蟲屬(Criconemella)物種、似環線蟲(Criconemoide)物種、 中環線蟲屬(Mesocriconema)物種;球莖線蟲(Stem and bulb nematode)、馬鈴薯腐敗線蟲(Ditylenchus destructor)、玉米莖線蟲(Ditylenchus dipsaci)及其他雙塾 刃屬(Ditylenchus)物種;錐線蟲(Awl nema-tode)、錐線蟲 屬(Dolichodorus)物種;螺旋形線蟲(Spiral nematode)、螺 旋形線蟲(Heliocotylenchus multicinctus)及其他螺旋線蟲 (Helicotylenchus)物種;鞘線蟲(Sheath and sheathoid nematode)、鞘線蟲屬(Hemicycliophora)物種及朝線蟲屬 (Hemicriconemoides)物種;潛根線蟲(Hirshmanniella)物 種;搶線蟲(Lance nematode)、冠線蟲(Hoploaimus)物種; 假根癭·線蟲(false rootknot nematode)、珍珠線蟲屬 (Nacobbus)物種;針線蟲(Needle nematode)、裂尾劍線蟲 (Longidorus elongatus)及其他長針線蟲屬(Longidorus)物 13366 丨.doc -114- 200917962 種;釘線蟲(Pin nematode)、擬墊刃屬(Paratylen-chus)物 種;損害線蟲(Lesion nematode)、加州根腐線蟲 (Pratylenchus neglectus)、穿刺短體線蟲(Pratylenchus penetrans)、彎曲短體線蟲(Pratylenchus curvitatus)、古德 依短體線蟲(Pratylenchus goodeyi)及其他根腐線蟲 (Pratylenchus)物種;穿孔線蟲(Burrowing nematode)、掘 穴線蟲(Radopholus similis)及其他内侵線蟲屬(Radopholus) 物種;腎形線蟲(Reniform nematode)、旋形線蟲 (Rotylenchus robustus)及其他盤旋線蟲屬(Rotylenchus)物 種;盾狀線蟲屬(Scutellonema)物種;殘根線蟲(Stubby root nematode)、克伯氏殘根線蟲(Trichodorus primitivus) 及其他殘根線蟲(Trichodorus)物種、擬毛刺線蟲 (Paratrichodorus)物種;短小線蟲(Stunt nematode)、克萊 頓矮化線蟲(Tylenchorhynchus claytoni)、不定矯化線蟲 (Tylenchorhynchus dubius)及其他接化線蟲屬 (Tylenchorhynchus)物種;桔線蟲(Citrus nematode)、柑橘 線蟲(Tylenchulus)物種;短劍線蟲(Dagger nematode)、臺 灣劍線蟲屬(Xiphinema)物種;及其他植物寄生性線蟲物 種。 在本發明較佳實施例中,式I或II化合物係用於控制昆蟲 或蜘蛛,尤其鱗翅目、鞘翅目、纓翅目及同翅目昆蟲及蜱 蜗目物蛛。本發明式I或II化合物尤其可用於控制缕翅目及 同翅目昆蟲。 式I或II化合物或包含其之殺蟲組合物可用於藉由使植 133661.doc •115· 200917962 物/作物與殺蟲有效量之式I或II化合物接觸來保護生長中 之植物及作物免受無脊椎害蟲(尤其昆蟲、蜗蟲或4知蛛)侵 襲或侵擾。術語”作物”指生長中之作物及已收穫之作物二 者。 式I或II化合物可轉化成常規調配物,例如溶液、乳液、 懸浮液、粉末、粉劑、膏劑及顆粒。應用形式取決於具體 既定目的;在每種情況下,皆應確保本發明化合物能夠精 細且均勻地分佈。 調配物可以已知方式來製備(綜述參見(例如)美國專利第 3,060,084號、歐洲專利第EP-A 707 445號(關於液體濃縮 物)、Browning, &quot;Agglomeration”,Chemical Engineering, 1967 年 12 月 4 日,147-48,Perry's Chemical Engineer's Handbook,第 4版,McGraw-Hill, New York, 1963,第 8, 57頁及以下文獻:WO 91/13546、美國專利第4,172,714 號、美國專利第4,144,050號、美國專利第3,920,442號、美 國專利第5,180,587號、美國專利第5,232,701號、美國專利 第5,208,030號、英國專利第2,095,558號、美國專利第 3,299,566號、Klingman, Weed Control as a Science, John Wiley and Sons公司,New York, 1961、Hance等人,Weed Control Handbook ,第 8 版,Blackwell Scientific Publications,Oxford, 1989 及 Mollet,H., Grubemann,A., Formulation tech-nology, Wiley VCH Verlag GmbH, Weinheim (Germany), 2001 ' 2. D. A. Knowles, Chemistry and Technology of Agrochemical Formulations, Kluwer 133661.doc -116- 200917962 ,1998 (ISBN 0-7514-0443-Preparation by the method described in ChemiStry 1989, 3 70, 1 7-3 i In general, the compound of formula 1 or hydrazine can be prepared by the above method. If the individual compounds are not prepared by the above routes, they can be prepared by other compounds or waxes by conventional changes to the synthetic route. By way of example, in some cases, 'some compounds I 哎 and 11 may advantageously be derived from other compounds I or by ester hydrolysis, amide amination, sulphation, cleavage, thinning, emulsification and the like. II to prepare. The reaction mixture can be treated in a conventional manner, for example by mixing with water, separating the phases and, if appropriate, purifying the crude product by chromatography (e.g., on Oxide or Shihua). Some intermediates and final products can be obtained in the form of colorless or light-colored viscous oils. They are freed from volatile components at low pressure and moderate vapority. If the intermediates and final products are obtained in the form of solids, 彳θ &amp; π ^ short oxime, they can be purified by recrystallization or grinding. Since the formula compound has (4) (iv) activity, it can be used to control invertebrate pests. Accordingly, the present invention also provides a method of controlling an invertebrate pest, the method comprising treating a scorpion moth with a pesticidally effective amount of a compound of the formula (1) or (π) as defined above or a salt or cerium-oxide or composition thereof Food supply, its habitat or its breeding grounds, or cultivated plants, planting materials (such as seeds), soils, soils, soils, fields, materials or environments, or To prevent I33661.doc 200917962 from invading or infesting pests, cultivated plants, plant propagation materials (such as seeds), soil, surface or space. Preferably, the method of the invention is used to protect plant propagation material (such as seeds) and plants grown therefrom from invading or infestation by invertebrate pests, and comprises formula (1) as defined above or (I] t) The compound or planting material (e.g., seed) may be treated with the agricultural composition as defined by the compound or its agriculturally acceptable salt or N-oxide or in the context of an insecticidally effective amount; The method of the invention is not limited to the protection of "matrices" (plants, plant propagation materials, soil materials, etc.) which have been treated according to the invention, and thus also for the growth of plants from treated plant propagation material (for example seeds) Sexual effects (eg protection from treated plant propagation material), in which the plant itself is not sunk, and 5, & spinal pests &quot; preferably selected from arthropods and nematodes' It is selected from harmful insects, spiders and nematodes, and even more preferably one is selected from the group consisting of insects, aphids and nematodes. V. b. The U.S. provides for the protection of the invertebrate pests, which contain at least a compound of an effective amount of insecticidal action, or a compound of at least one of the agriculturally available salt silk oxides, and At least one liquid and/or solid inert carrier, and, if desired, at least one surfactant. According to the invention, the composition may comprise a mono-active formula or a compound or a dish or an N-oxide &lt; a right-drying active compound! or a mixture of η or a salt thereof. The present invention may comprise a separate aliquot. Isomers or mixtures of isomers and mixtures of individual tautomers or tautomers. 133661 .doc -104· 200917962 Compounds of formula I or II and insecticidal compositions comprising same thereof control arthropod pests and nematodes An effective agent. Invertebrate worms controlled by a compound of formula I or II include, for example: from Lepidoptera (Lepidoptera, such as small tigers (dgro, yellow tiger) (Jgro, cotton leaf moth) , Lima nocturnal gemwaia/b), apple nest moth co^/wge//a), scorpion worm (Jwiograp/m gamma), pine stalk (5wpa/w5·piWari.ws), fir rough Moth (Cacoecia mwr/nanci) 'Capwa reiicw/ana, winter moth (C/zez·βίοΜα 6rwm&lt;aia), spruce leaf moth {Choristoneura fumiferana), western spruce leaf moth {Choristoneura occidentalis), beauty; ί, state poison worm (Cirphis, apple 蠹(C_y mountain, European pine caterpillar [Dendrolimus pini], melon ff 嗓 {Diaphania nitidalis), 良良米米 [Diatraea, Egyptian vajra 五 (five/like insulana) &gt; South American jade snail snail [Elasmopalpus lignosellus ), Eupoecilia ambiguella 'Evetria bouliana, Feltia subterranea, Galleria mellonella' Graphogitha funebrana, pear "Grapholitha molesta", Heliothis armigera, Heliothis virescens, Heliothis zea, Hellula undalis, Hebrew moth (// 76erm_a c?e/o/i'an_a), American white moth (//_yp/zanir/c! cwnea), apple moth (if_yponc&gt;mewia, 蠹 蠹 133 133661.doc -105- 200917962 {Keiferia lycopersicella) '{Lambdina fiscellaria) 'Beet armyworm exigua), coffee point moth (coffeella), stalking moth ^ {Leucoptera, snail moth {Lithocolletis, Zobeha 6oircma, yellow green scorpion (Loxcmege Siiciica/b), "Lymantria dispar" ' it ^ ^ ^{Lymantria monacha) ' Narrow-winged leaf miner (L_yo«e&quot;iJ! clerkellcT), canopy% QMalacosoma newwr/fl), cabbage moth (Mawairo;, cedar moth psewiioiswgaia ), European corn mold (〇5/W«z_a wwW/flD), winter night moth QPanolis flammea), title [Pectinophora and pie//a), Beans hornworm, 'Phalera bucephala' , Ma Ling integrated 1 weaving (Phthorimaea opercw / eZ / a), orange fine moth cz7re / / a), large cabbage moth, 苜 绿 green night moth (Ρ / αί / ζ less / 7 (9) a, Plutella xylostella {Plutella Xylostella), Soybean larvae (Pseudoplusia, Lobster leaf moth (/?/z_yaciom'a / rwsirawa), Svelbipalpula absoluta, Sitobiga cerealella, S. cerevisiae (Sparganoi) /ib ρί//6η·α«α), Spodoptera frugiperda, Spodo/opiem littoralis, Spodoptera litura (*S/7〇i/〇/&gt;iera / Z'iwrcz), J'haumatopoea pityocampa 'Tortrix viridana', Tyichoplusia «/·) and the cloud {Zeiraphera canadensis) » Aphids (Coleoptera), such as pear long ginkdin (Agrilus -106-133661.doc 200917962 sinuatus), Agriotes lineatus, dark-skinned 0P armor Agriotes obscurus), Amphimallus solstitialis, Anisandrus dispar, Anthonomus grandis, Anthonomus pomorum, Atomaria linearis, Dasong Blastophagus piniperda, Blit'ophaga undata, Bruchus runmanus, Bruchus pisorum, Bruchus lentis, Rhododendron lobes Byetiscus betulae., Cesida nebulosa, Cerotoma trifurcata, Ceuthorrhynchus assimilis, Ceuthorrhynchus napi, Chaetoenema tibialis, Tobacco Needles Conoderus vespertinus, Crioceris asparagi, Diabrotica longicornis, Diabrotica 12-punctata), Diabrotica virgifera, Epilachna varivestis, Epitrix hirtipennis, Eutinbothrus brasiliensis, Hylobius abietis, Egyptian elephant Yp (Hypera brunneipennis), Hypera postica, Ips typographus, Lema bilineata, Lema melanopus, potato beetle Leptinotarsa decemlineata), Limonius californicus, Lissorhoptrus oryzophilus, Melanotus communis, Meligethes aeneus, and Melodontha 133661.doc •107· 200917962 hippocastani), European tortoise (Melolontha melolontha), Oulema oryzae, Ortiorrhynchus sulcatus, Otiorrhynchus ovatus, Phaedon cochleariae, Phyllantreta chrysocephala, Phyllophaga sp., garden Phyllopertha horticola, Phyllotreta nemorum, Phyllotreta striolata, Popillia japonica, Sitona lineatus, and Sitophilus granaria; Winged insects (Diptera, such as Aedes aegypti, Aedes aegypti), Anastrepha ludens, Anopheles maculipennis, Mediterranean rope (Cerai / 、, sister gold 13⁄4 bezziana) 'Spiral gold rope (C/zrpowya; 7〇wz'm_vora; c), Chrysomya macellaria, Contarinia sorghicolcT, Cordylobia anthropophaga, Culex pipiens Cw/ex Dacwj cwcwrZn7ae, Dacw 〇/eae, Brassica oleracea, yellow-bellied reins (Fa (four) ζ_α cam'cw/arb), bots {Gasterophilusintestinalis, ^^ i^, Glossinamorsitans, Haematobia irritans, Haplodiplosis e-wairh, species radiance | p/aiwro, mosquito cord, Zz'r/omyza saii' Vae), Africa Chrysanthemum (Liriomyza's /o/H), Lepidopteran (Lwcz'&quot;a (10)), Brassica 133661.doc •108- 200917962 (Lucilia cuprina) 'Luciiia sericata', jade neck Musca domestica (Μαγη·ο/α AWrwcior), Musca domestica (Mwca 廄 廄 ( (Mwscka wMw/a), Sheep Swine (Oairw·? ovk), Swedish wheat fly y&gt;&quot; ), beet leaf miner (Pegomya / zwoc awz·), onion fly a/7&quot; "wa", broccoli fly (P/zorha ^ a MZ'cae), wheat fly (p; 2〇rHa coarciak) , cherry fruit fly (sweet 0/如··? ceran'), apple fruit fly (sigh sigh / e mountain pomonella), ^ it (Tabanus bovinus) 'sweep big mosquito (TipuZa oleracea): ^ Huan if\\ Big mosquito [Tipula paludosa&quot;) ·, hummer (77〇^«opiera), such as Dichromothrips corbetti, Frankliniella / wsca, FrimWm e//a occWenia/b), Frankliniella tritici, Scirtothrips citrV, rice Suma (Γ/2η&gt;·5 or less zae), palm hummer (77zrz&gt;s pa /m/) and cotton aphid {Thrips tabaci); Hymenoptera (Hymenoptera), such as Athalia rosae, Atta cephalotes, Atta sexdens, and Atta texana ), Hoplocampa minuta, Hoplocampa testudinea, Monomorium pharaonis, Solenopsis geminata, and Solenopsis invicta; Isoparms (Hymenoptera) (Heteroptera)), such as Acrosternum hilare, Blissus leucopterus, Cyrtopeltis notatus, Dysdercus cingulatus, 133661.doc -109- 200917962 (Dysdercus intermedius), Eurygaster integriceps, Euschistus impictiventris, Leptoglossus phyllopus, Lygus lineolaris, Lygus pratensis, rice green Wall (Nezara viridula), Pesma quadrata, Solubea insularis and Thyanta perditor; Homoptera (//omopiera), such as red bean ({Acyrthosiphon onobrychis), larch ball (Jc/e/gei laricis), Aphidula nasturtii, Aphis / a6ae, strawberry roots , apple money, cotton money gowypH), gooseberry teeth groww/arz'ae), tea money (/ip/zz··? sc/meWerz·), 缭线菊财(/ίρ/π··?, bone Aphis sambuci, Acyrthosiphon pisum, % gully without web (Aulacorthum · 5〇/α«〇, silver leaf powder chaos (square emb/a, Bemisia tabaci), short Brachycaudus cardui &gt; Lee Macaque 蚜/2e/k/2r less d), Prunus cereus s pem'cae), Pruene koala 蚜, 甘 raw/cae)角钉毛财 (Caphop/zorws /zorm·), cotton winged net bee (Cerosipha gossypii), 萆berry hair f 蚜 (chaetosiphon, life 蘼 蘼 额 额 ( (Cryp/om less r/Ws), Caucasian spheroid (Drey/wha nordmannianae) 'Sycamore vertebrate (Drey/MWa, Ryd Koala round tail ra::/z'c〇/a), Dysaulacorthum psewdosolani, 鳋Pink 蚜 ( Dysaphis 133661.do C -110- 200917962 (10)), Pythium pygma pyW), Empoasca fabae, Hyalopterus pruni, tea vines (i/xperomj/zws lactu-cae), ginseng f Macrosiphum avewae, Macrosz'p/zwm ewp/zorb/ae, Macrohp/^ow rosae, Megahoura Wc/ae, Paloese彩财(Me/awap/n's, 麦麦麦财{Met opol op hi um dirhodum), ^ {Myzodes persicae) 'Myzws c^ca/oWcw', 黑 cherry melanoma (蚜) (10) cerah ), peach aphid (M_yzWly perhC (3e), nuclear xanthoma fronto (from a small heart var/aw), wormwood (iVa>so«ov/a, brown rice bran (w/a_parvaia /wge) , 万 根 6 6 6wriyar? 'Wi5), cane toad (Perh « _e / / a Mcc / mricWa), Python 疣 疣 (P; / 〇r0t / o « do www / z ') , Ping Mufeng (corpse sy/Za Wa//), pear wood milk (corpse π//α pirz·), winter onion tumor 蚜 {Rhopalomyzus ascalonicus), corn tuber 蚜 {Rhopalosiphum maidis, 缢 缢 缢 ( Rhopa丨osiphum /?ac^·), Yu Liyi tube 蚜insertum), pear stone Grass (Sappaphis wa / a), Doberan red round tail wealth Wa / z ·), Mai two and 蚜 (Schizaphis grawkwm), Avocado cotton jacket (Sc / n.zc ^ ewra / (10) wg / wow), Mai Chang Tube (&amp;·/〇&amp;·〇« this), white backed fly {Sogatella / wrcz/era), greenhouse whitefly (JWa/ewoc/w vaporar/orww), orange two (7\? ;c〇/^era awr&lt;a«&quot;i·) and the grape root nodule field [Viteus vitifolii]', white pelicans (Isoptera), such as the European wood white sacrifice (Calotermes flavicollis), European and American termites ( Leucotermes flavipes), yellow-breasted white 133661.doc -111 - 200917962 Ant (Reticulitermes flavipes), Reticuiitermes lucifugus and Termes natalensis; Orthoptera (Orthoptera (Ori/zop(10)α) ), for example, JadeM ί/owai/ca, Oriental Filipino (β/α&quot;α or/ewiaD), Blattella germanica, Forficula auricularia, GryHoiaipa Gryn〇ta!pa), Loewsk wz'grofMWa, double belt Me (Me/a«op/WlS 赤腿蚱蜢(Melanoplus femurrubrum), 墨西蛑蜢 (Melanoplus, Me/a/iop/ws, Melanoplus spretus, m (Nomadacris septemfasciata), American cockroach (Perz&gt;/(d) ek ameWc (four) α), American 蚱amehca« a), Paregrina 蚱蜢 (10)), Stauronotus and greenhouse 蟋螽 (rac / 〇; cz ^ asynamorus); Arachnida (Aflc / moz · heart a) 'eg spider (蜱螨 ycar / wa)) For example, the soft scorpion (drgim·e and e), the hard scorpion (/x〇i/wae), and the scorpion (~rC〇Jp&quot;· and e) 'for example, the American flower 蜱 矽 10 (10) ame ameWc (10) , tropical flower bud (dm6/_yowma vaWegaiwm), Persian concealed (^ is like perWcws), with square head 蜱 (10) (10),), Boophilus decoloratus, micro + burdock iBoophilus micr〇plus, , forest leather 蜱 (Der _s / / varww), long &quot; glazed eyelids (/% / (10) brain, scorpion hard 蜱 (/ ΧΟύ ^ rycz · " (10)), light red hard 蜱 (^^ Heart ^ rubicundus), rabbit office (_〇rnithodorus moubata) 'disability.缉 缉 (Oiohw meg (1)· "/), chicken skin hedgehog (Der-machi to (10) / / i > me), sheep 133661.doc -112- 200917962 pain (Psoroptes ovis) 'tail M monument (Rkipicephalus mountain 'cw/aiws), valgus fan head 蜱ever/), acne worm height ("Sarcopie5·ααά/β/) and 瘿 瘿 ( (5 Hop/zyzWae spp.), such as 瘿 瘿 瘿 (yicw/ Ws ίΆ/π/7ίβ«ΰ?β/ζ·), orange rust (P/z&gt;&gt;//oc;o/?iraia o/e/vora) and citrus buds (five riop/zyes s /ze/i/om·); tree line 瞒科 (Γααο plus w/dae sppj, such as cyclamen snail (corpse / z_yicmemwj pallidus) anti-multiple food woven fabric (Polyphagotarsonemus latus) ·, pseudo-leaf family 7&gt;«Μφα^αίαβ spp.), such as the purple pseudo-leaf (BreWpa/pw p/zoem'cb); the leaf family (7&gt;ira^yc/H'c/(3e 577/?·), such as cinnabar ·Ye worm (reira^yc/zz^ cz'(10)Marz'wws), Shenze's leaf 螨Α: ϊ ζ ζ ν 太平洋 、 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋 太平洋«_yc/2ws ie/arks) and cotton leaf wri/cae), apple full claw 螨 w/w〇, orange full claw 螨 like cz'in') and grass small claw worm ongo / ^ c ^ ws praiewb); Siphonaptera (Siphonatera) 'oriental rat flea e.g. (Xenopsylla cheopsis), the genus Ceratophyllus flea (Ceratophyllus spp).. The composition and the compound of formula I or II can be used to control nematodes, especially plant-parasitic nematodes, such as root knot nematode, Meloidogyne hapla, Meloidogyne incognita, and root-knot nematode (Meloidogyne javanica), and other Meloidogyne species; cyst-forming nematode, Globodera rostochiensis, and other Globodera species; oat cyst nematode (Het) -erodera avenae), soybean cyst nematode 133661.doc •113· 200917962 (Heterodera glycines), beet cyst nematode (Heterodera schachtii), cystosome nematode (Heterodera trifolii), and other cystic nematodes (Heterodera) species; Seed gall nematode, Anguina species; Stem and foliar nematode, Aphelenchoide species; Sting nematode, Belonolaimus longicaudatus And other species of the beetle nematode (Belonolaimus); Pine nematode, Bursaphelenchus xylophilus and other species of Bursaphelenchus; Ring nematode, Criconema species, Criconemella species, Criconemoide species, Central Mesocriconema species; Stem and bulb nematode, Ditylenchus destructor, Ditylenchus dipsaci and other Ditylenchus species; Cone nematodes (Awl nema-tode) , the species of the genus Dolichodorus; Spiral nematode, Heliocotylenchus multicinctus and other species of Helicotyllenchus; Sheath and sheathoid nematode, Hemicycliophora species and Hemicriconemoides species; Hirshmanniella species; Lance nematode, Hoploaimus species; false rootknot nematode, Nacobbus species; Nematode (Needle nematode), crack Longidorus elongatus and other Longidorus 13366 丨.doc -114- 200917962 species; Pin nematode, Paratylen-chus species; Lesion nematode, Pratylenchus neglectus, Pratylenchus penetrans, Pratylenchus curvitatus, Pratylenchus goodeyi, and other root rot nematodes (Pratylenchus) species; perforated nematodes ( Burrowing nematode), Radopholus similis and other Radopholus species; Reniform nematode, Rotylenchus robustus and other Rotylenchus species; Scutellonema species; Stubby root nematode, Trichodorus primitivus and other Trichodorus species, Paratrichodorus species; Stunt nematode, Clayton dwarf nematode (Tylenchorhynchus claytoni), indefinite orthodontic Tylenchorhynchus dubius and other species of the genus Tylenchorhynchus; Citrus nematode, Tylenchulus species; Dagger nematode, Taiwanese Xiphinema species; and other plants Parasitic nematode species. In a preferred embodiment of the invention, the compound of formula I or II is used to control insects or spiders, particularly Lepidoptera, Coleoptera, Thysanoptera, and Homoptera and Cocoon. The compounds of the formula I or II according to the invention are especially useful for controlling Thysanoptera and Homoptera insects. The compound of formula I or II or a pesticidal composition comprising the same can be used to protect growing plants and crops by contacting the plant 133661.doc • 115· 200917962/crop with a pesticidally effective amount of a compound of formula I or II. Infested or infested by invertebrate pests (especially insects, worms or spiders). The term "crop" refers to both growing crops and harvested crops. The compounds of formula I or II can be converted into conventional formulations such as solutions, emulsions, suspensions, powders, powders, pastes and granules. The form of application depends on the specific intended purpose; in each case, it should be ensured that the compounds of the invention are capable of being finely and uniformly distributed. Formulations can be prepared in a known manner (for review, see, for example, U.S. Patent No. 3,060,084, European Patent No. EP-A 707 445 (with regard to liquid concentrates), Browning, &quot;Agglomeration", Chemical Engineering, December 1967 4th, 147-48, Perry's Chemical Engineer's Handbook, 4th edition, McGraw-Hill, New York, 1963, pp. 8, 57 and below: WO 91/13546, U.S. Patent No. 4,172,714, U.S. Patent No. 4, 144,050, U.S. Patent No. 3,920,442, U.S. Patent No. 5,180,587, U.S. Patent No. 5,232,701, U.S. Patent No. 5,208,030, U.S. Patent No. 2,095,558, U.S. Patent No. 3,299,566, Klingman, Weed Control as a Science, John Wiley and Sons, New York, 1961, Hance et al., Weed Control Handbook, 8th Ed., Blackwell Scientific Publications, Oxford, 1989 and Mollet, H., Grubemann, A., Formulation tech-nology, Wiley VCH Verlag GmbH, Weinheim (Germany), 2001 ' 2. DA Knowles, Chemistry and Technology of Agrochemical Formulations, Kluwer 133661.do C -116- 200917962 ,1998 (ISBN 0-7514-0443-

適宜溶劑之實例為水、芳香族溶劑(例如SGlvess〇產品Examples of suitable solvents are water, aromatic solvents (eg SGlvess® products)

Academic Publishers, Dordrecht, 1998 8)),例如藉由將適用於調配農用化學 劑及/或載劑,(若需要)乳化劑、表面〉: 甲D、石堪(例如礦物油偷厶、、高言来s / μ , m _Academic Publishers, Dordrecht, 1998 8)), for example by applying an agrochemical and/or carrier, if necessary, an emulsifier, surface >: A D, Shi Kan (eg mineral oil stealing, high)言 / s , m _

適且礼化劑為非離子型及陰離子型乳化劑(例如聚氧乙 烯脂肪醇醚、烷基磺酸鹽及芳基磺酸鹽)。 分散劑之實例為木素-亞硫酸鹽廢液及甲基纖維素。 所用適宜表面活性劑為木質素磺酸、萘磺酸、酚基磺 酸、二丁基萘磺酸、烷基芳基磺酸酯、烷基硫酸酯、烷基 磺酸酯、脂肪醇硫酸酯、脂肪酸及硫酸化脂肪醇二醇醚之 鹼金屬、鹼土金屬及銨鹽;以及磺酸化萘及萘衍生物與曱 醒之縮合物、萘或萘磺酸與苯酚及曱醛之縮合物、聚氧乙 稀辛基紛醚、乙氧基化異辛基酚、辛基酚、壬基酚、烷基 酚聚乙二醇醚、三丁基苯基聚乙二醇醚、三硬脂基苯基聚 乙二醇醚、烷基芳基聚醚醇、醇及脂肪醇/環氧乙烷縮合 物、乙氧基化蓖麻油、聚氧乙烯烷基醚;乙氧基化聚氧丙 133661.doc -117- 200917962 :,、月桂醇聚乙二醇醚縮醛、山梨醇酯、纟質素亞硫酸鹽 廢液及甲基纖維素。 ,於製備可直接嘴灑之溶液、乳液、膏劑或油分散液之 勿貝係具有中至高沸點之礦物油餾分,例如煤油或柴油, 、、’、、“由及植物〆由或動物油' 脂肪煙、環煙及芳烴,例 女口 ^ —甲苯、石蠟、四氫化萘、烷基化萘或其衍生 物、甲醇、乙醇、丙 _ % 丁知、裱己醇、環己酮、異佛爾 酮、高極性溶劑,例 _ H 列如一甲基亞硬、N-甲基吡咯啶酮或 水。 亦可將諸如甘油、7 ^ 乙一醇、丙二醇等防凍劑及殺細菌劑 加入調配物中。 適且消泡劑為(例如)基於矽或硬脂酸鎂之消泡劑。 適宜防腐劑為(例如)雙氯酚。 種子處理6周配物可另外包含黏合劑與(視需要)著色劑。 可添加黏合劑以改良處理後活性材料在種子上之黏著。 適宜黏合劑係嵌段共聚物EO/PO表面活性劑,亦及聚乙稀 醇、聚乙烤&quot;比洛°定酮、聚丙烤酸Θ旨、聚甲基丙稀酸醋、聚 丁烯$異丁烯、聚苯乙烯、聚乙烯胺、$乙烯醯胺、聚 乙烯亞胺(LUpas〇i®、P〇lymin⑧)、聚醚、聚胺基曱酸酯、 聚乙稀乙酸酿、甲基纖維素(tylose)及衍生自該等聚合物之 共聚物。 視需要,著色劑亦可包括於調配物中。用於種子處理調 配物之適宜著色劑或染料係羅丹明B(Rhodamin B)、C.I.顏 料紅112、C.I·溶劑紅丨、顏料藍15:4、顏料藍15:3、顏料藍 133661.doc -118- 200917962 顏料藍1 5,1、顏料藍8 〇、顏料黃1、顏料黃1 3、顏料 紅112、顏料紅48:2、顏料紅48:1、顏料紅57:1、顏料紅 顏料撥43、顏料橙34、顏料撥5、顏料綠3 6、顏料 綠7、顏料白6、顏料棕25、鹼性紫10、鹼性紫49、酸性紅 5 1、酸性紅52、酸性紅14、酸性藍9、酸性黃23、鹼性紅 1 〇、鹼性紅1 〇 8。 膠凝劑實例為角又菜(Satiagel(g))。 粉劑(即用於撒布之材料及可撒施產物)可藉由混合或同 時研磨活性物質與固體載劑來製備。 藉由將活性化合物黏合至固體載劑來製備顆粒,例如經 塗佈顆粒、經浸潰顆粒及均質顆粒。 固體載劑之實例係礦物土(例如矽膠、矽酸鹽、滑石 粉、高嶺土、美國活性白土(attaclay)、石灰石、石灰、白 堊、紅玄武土、黃土、黏土、白雲石、矽藻土、硫酸鈣、 硫酸鎂、氧化鎂、經研磨合成材料)、肥料(例如硫酸銨、 麟酸敍、石肖酸銨、尿素)及植物源產物(例如穀類粗粉、樹 皮粗粉、木粉及堅果殼粗粉)、纖維素粉末及其他固體載 劑。 一般而言,調配物包含0.01_95重量%、較佳〇丨—90重量 %之活性化合物。在此情況下,_活性化合物之純度係 介於90重量%至100重量%之間,車交佳介於95重量%至1〇〇 重量%之間(根據NMR譜)。 出於種子處理目的,可將各調配物稀釋2至1〇倍以使即 用製劑中活性化合物之重量比濃度介於q q i _ 6 g重量%之 133661.doc -119- 200917962 間,較佳介於0 · 1 - 4 0重量%之。 式1或Π化合物可藉由噴灑、喷霧、撒施、撒布或灌注方 式以其調配物形式或自其製備之使用形式原樣使用,例如 可直接喷灑之溶液、粉劑、懸浮液或分散液、乳液1分 散液、膏劑、可撒施產物、撒布用材料、或顆粒形式。使 用形式完全取決於既定目的;意欲在每一情況下確保本發 明活性化合物可達成盡可能最精細之分佈。 可藉由添加水自乳液濃縮物、膏劑或可濕性粉劑(可噴 麗粉劑、油分散液)製備水性使用形式。為製備乳劑、客 劑或油分散液,可藉由潤濕劑、膠黏劑、分散劑或乳化: 在水中使未經處理的或溶於油或溶劑中之物質均質化。狹 而,亦可能製備由活性物質、潤濕劑、膠黏劑、分散劑 礼化劑及(若適宜)溶劑或油組成之濃縮物,且該等濃縮物 適於用水稀釋。 即用製劑中活性化合物之濃度可在相對寬範圍内變化。 通常’此濃度以重#計係〇.__1()%,較佳 活性化合物亦可成功地用於超低量方法(ulv)中,可施 用:含95重量%以上活性化合物之調配物,或甚至可施用 不含添加劑之活性化合物。 下文為調配物之實例: L葉片施用的用水稀釋之產物。出於種子處理目的,可 以稀釋或未稀釋形式將該等產物施用至種子上。 A)水溶性濃縮物(SL、LS) 使1〇重量份數活性化合物溶於9〇重量份數水或水溶性溶 133661.doc -120- 200917962 w中。作為替代方案’可添加潤濕劑或其他輔助劑。用水 稀釋後活性化合物溶解’藉此獲得含有丨〇% (w/w)活性化 合物之調配物。 B)可分散濃縮物(DC) 使20重量份數活性化合物溶於7〇重量份數環己酮中,並 添加1 0重量份數分散劑(例如聚乙烯D比略咬酮)。用水稀釋 來得到分散液,藉此獲得含20% (W/W)活性化合物之調配 物。 c)可乳化濃縮物(EC) 使15重量份數活性化合物在添加十二烷基苯磺酸鈣及乙 氧基化蓖麻油(各自添加5重量份數)下溶於7重量份數二甲 苯中。用水稀釋而得到乳液,藉此獲得含有15% (w/句活 性化合物之調配物。 D)乳液(EW、EO、ES)Suitable emulsifiers are nonionic and anionic emulsifiers (e.g., polyoxyethylene fatty alcohol ethers, alkyl sulfonates, and aryl sulfonates). Examples of dispersing agents are lignin-sulfite waste liquors and methylcellulose. Suitable surfactants used are lignosulfonic acid, naphthalenesulfonic acid, phenolsulfonic acid, dibutylnaphthalenesulfonic acid, alkylarylsulfonate, alkylsulfate, alkylsulfonate, fatty alcohol sulfate , alkali metal, alkaline earth metal and ammonium salt of fatty acid and sulfated fatty alcohol glycol ether; and condensate of sulfonated naphthalene and naphthalene derivatives with awakening, condensate of naphthalene or naphthalenesulfonic acid with phenol and furfural, poly Oxyethylene octyl ether, ethoxylated isooctyl phenol, octyl phenol, nonyl phenol, alkyl phenol polyglycol ether, tributyl phenyl polyglycol ether, tristearyl benzene Polyglycol ether, alkyl aryl polyether alcohol, alcohol and fatty alcohol / ethylene oxide condensate, ethoxylated castor oil, polyoxyethylene alkyl ether; ethoxylated polyoxypropylene 133661. Doc -117- 200917962 :,, lauryl alcohol polyglycol ether acetal, sorbitol ester, bismuth sulfite waste liquid and methyl cellulose. , in the preparation of a solution, emulsion, ointment or oil dispersion which can be directly sprinkled, has a medium to high boiling mineral oil fraction, such as kerosene or diesel, ',, 'from and plant 〆 or animal oil' fat Smoke, ring smoke and aromatic hydrocarbons, such as female mouth - toluene, paraffin, tetrahydronaphthalene, alkylated naphthalene or its derivatives, methanol, ethanol, propylene _ % butyl, hexanol, cyclohexanone, isophor Ketones, highly polar solvents, such as _H column such as monomethyl hard, N-methylpyrrolidone or water. Antifreezes such as glycerin, 7^-ethyl alcohol, propylene glycol, and bactericides may also be added to the formulation. Suitable antifoaming agents are, for example, antifoaming agents based on strontium or magnesium stearate. Suitable preservatives are, for example, dichlorophenol. Seed treatment for 6 weeks may additionally comprise binders and (as needed) colorants Adhesive may be added to improve the adhesion of the active material to the seed after treatment. Suitable binder is block copolymer EO/PO surfactant, and also polyethylene glycol, polyb-baked &quot;Bilobutanone, Polypropylene roasting acid, polymethyl acrylate vinegar, polybutene , polystyrene, polyvinylamine, vinyl amide, polyethyleneimine (LUpas〇i®, P〇lymin8), polyether, polyamine phthalate, polyethylene acetate, methyl cellulose ( Tylose) and copolymers derived from such polymers. Colorants may also be included in the formulation, as appropriate. Suitable colorants or dyes for seed treatment formulations are Rhodamin B, CI Pigment Red. 112, CI·solvent red hydrazine, pigment blue 15:4, pigment blue 15:3, pigment blue 133661.doc -118- 200917962 Pigment blue 1 5, 1, pigment blue 8 〇, pigment yellow 1, pigment yellow 1 3, Pigment red 112, pigment red 48:2, pigment red 48:1, pigment red 57:1, pigment red pigment dial 43, pigment orange 34, pigment dial 5, pigment green 3 6, pigment green 7, pigment white 6, pigment Brown 25, alkaline violet 10, basic violet 49, acid red 5 1, acid red 52, acid red 14, acid blue 9, acid yellow 23, alkaline red 1 碱性, alkaline red 1 〇 8. Gelling agent An example is Satiegel (g). A powder (ie, a material for spreading and a spreadable product) can be prepared by mixing or simultaneously grinding the active material with a solid carrier. Particles are prepared by binding the active compound to a solid carrier, such as coated particles, impregnated particles, and homogeneous particles. Examples of solid carriers are mineral soils (eg, silicone, silicate, talc, kaolin, American activated clay (attaclay), limestone, lime, chalk, red basalt, loess, clay, dolomite, diatomaceous earth, calcium sulfate, magnesium sulfate, magnesium oxide, ground synthetic materials), fertilizer (such as ammonium sulfate, Lin Acidic, ammonium sulphate, urea) and plant-derived products (such as cereal meal, bark meal, wood flour and nutshell meal), cellulose powder and other solid carriers. In general, the formulation comprises from 0.01% to 95% by weight, preferably from 00% to 90% by weight, of the active compound. In this case, the purity of the active compound is between 90% and 100% by weight, and the car is preferably between 95% and 1% by weight (according to NMR spectrum). For seed treatment purposes, each formulation may be diluted 2 to 1 fold so that the weight ratio of active compound in the ready-to-use formulation is between qqi _ 6 g wt% 133661.doc -119- 200917962, preferably between 0 · 1 - 40 0% by weight. The formula 1 or the hydrazine compound can be used as it is by spraying, spraying, spreading, spreading or perfusion in the form of its formulation or the form prepared therefrom, for example, a solution, a powder, a suspension or a dispersion which can be directly sprayed. , emulsion 1 dispersion, paste, spreadable product, spreading material, or granular form. The use form is entirely dependent on the intended purpose; it is intended to ensure, in each case, that the active compound of the invention achieves the finest possible distribution. The aqueous use form can be prepared by adding water from an emulsion concentrate, a paste or a wettable powder (a sprayable powder, an oil dispersion). For the preparation of emulsions, guest or oil dispersions, the materials which are untreated or dissolved in oil or solvent can be homogenized in water by means of wetting agents, adhesives, dispersants or emulsification. Narrowly, it is also possible to prepare concentrates consisting of active substances, wetting agents, adhesives, dispersing agents and, if appropriate, solvents or oils, and such concentrates are suitable for dilution with water. The concentration of the active compound in the ready-to-use formulations can vary over a relatively wide range. Usually, the concentration of the active compound is 〇.__1 (%), and the preferred active compound can also be successfully used in the ultra low amount method (ulv), and can be applied: a formulation containing more than 95% by weight of the active compound, or It is even possible to apply an active compound which does not contain an additive. The following are examples of formulations: The product of the L blade application diluted with water. These products can be applied to the seed in diluted or undiluted form for seed treatment purposes. A) Water-soluble concentrate (SL, LS) 1 part by weight of the active compound is dissolved in 9 parts by weight of water or water-soluble 133661.doc -120-200917962w. As an alternative, a wetting agent or other adjuvant may be added. The active compound is dissolved after dilution with water' to thereby obtain a formulation containing 丨〇% (w/w) of the active compound. B) Dispersible Concentrate (DC) 20 parts by weight of the active compound are dissolved in 7 parts by weight of cyclohexanone, and 10 parts by weight of a dispersing agent (e.g., polyethylene D to singeone) is added. The dispersion was diluted with water to obtain a formulation containing 20% (w/w) of the active compound. c) emulsifiable concentrate (EC) 15 parts by weight of the active compound dissolved in 7 parts by weight of xylene under the addition of calcium dodecylbenzenesulfonate and ethoxylated castor oil (each added 5 parts by weight) in. Dilute with water to obtain an emulsion, thereby obtaining a formulation containing 15% (w/active compound. D) emulsion (EW, EO, ES)

使25重量份數活性化合物溶於35重量份數二甲笨中,並 添加十二烷基苯磺酸鈣及乙氧基化萬麻油(各自添加5重量 份數)。藉由乳化機(例如Ultraturrax)方式將此混合物引入 ⑽重量份數水中並製成均質乳液。用水稀釋而得到乳液, 藉此獲得含2 5 °/〇 (w/w)活性化合物之調配物。 E)懸浮液(SC、〇D、FS) 在授抖1球磨機中,2 0重量份數之活 旦/八缸\玉 性化&amp;物於添加ιυ垔 ……、潤濕劑及70重量份數水或有機溶劑下粉 碎,以得到細緻之活性化合物料液 性化合物之穩定懸浮液,藉此獲得含有2二:::: 133661.doc 121 200917962 合物之調配物。 F)水可分散顆粒及水溶性顆粒(WG、SG) 於添加50重量份數分散劑及潤濕劑下細細地研磨50重量 份數活性化合物,並藉由技術設備(例如擠壓器、喷霧 塔、流化床)將其製成水可分散或水溶性顆粒。用水稀釋 而得到活性化合物之穩定分散液或溶液,藉此獲得含有 5〇°/。(w/w)活性化合物之調配物。25 parts by weight of the active compound was dissolved in 35 parts by weight of dimethyl sulfonate, and calcium dodecylbenzenesulfonate and ethoxylated cannabis oil (5 parts by weight each) were added. This mixture is introduced into (10) parts by weight of water by means of an emulsifier (e.g., Ultraturrax) to form a homogeneous emulsion. It is diluted with water to give an emulsion, whereby a formulation containing 25 ° / 〇 (w / w) of the active compound is obtained. E) Suspension (SC, 〇D, FS) In the shaker 1 ball mill, 20 parts by weight of live dan / eight cylinders \ jade &amp; add to ιυ垔..., wetting agent and 70 weight The mixture is pulverized in water or an organic solvent to obtain a stable suspension of the fine active compound liquid compound, whereby a formulation containing 2:::::133661.doc 121 200917962 is obtained. F) water-dispersible granules and water-soluble granules (WG, SG) finely grind 50 parts by weight of the active compound with the addition of 50 parts by weight of a dispersing agent and a wetting agent, and by means of technical equipment (for example, an extruder, The spray tower, fluidized bed) is made into water-dispersible or water-soluble particles. Dilution with water gives a stable dispersion or solution of the active compound, whereby it is obtained to contain 5 Å. (w/w) a formulation of the active compound.

G)水可分散粉劑及水溶性粉劑(WP、SP、SS、WS) 在添加25重量份數分散劑、潤濕劑及矽膠下於轉子-定 子磨機中研磨75重量份數活性化合物。用水稀釋而得到活 眭化合物之穩定分散液或溶液,藉此獲得含75°Λ (w/w)活 性化合物之調配物。 H)凝膠調配物(GF) 在攪拌球磨機中,於添加1 〇重量份數分散劑、1重量份 數勝凝劑㈤濕劑及70重量份數水或有機溶劑下,將2〇重量 份數活性化合物粉碎,以獲得細緻之活性化合物懸浮液。 用水稀釋而得到活性化合物之穩定懸浮液,藉此獲得含有 20% (w/w)活性化合物之調配物。 2·不經稀釋即用於葉片施用之產#。出於種子處理 的,可以稀釋或未稀釋形相該等產物施用至種子上。 U可撒施粉劑(DP、DS) 將5重量份數活性化人脱牲a 古 〇物精、、、田研磨並與95重量份數精 回嶺土充分混合。藉此得到 撒施產f 有W (Ww)活性化合物之 133661,doc -122· 200917962 J) 顆粒(GR、FG、GG、MG) 將0.5重量份數活性化合物精細研磨並與95 5重量份數載 背1J混合’藉此獲得含有〇. 5 % (w/w)活性化合物之調配物。 現行方法係擠出、喷霧乾燥或流化床。由此得到不經稀釋 即用於葉片應用之顆粒。 K) ULV溶液(UL) 使10重量份數活性化合物溶於9〇重量份數有機溶劑(例 如二甲苯)中。由此得到含1〇% (w/w)活性化合物之產物, 其可不經稀釋即用於葉片應用。 式Ϊ或II化合物亦適用於處理植物繁殖材料(例如種子)。 習知種子處理調配物包括(例如)可流動濃縮物FS、溶液 LS、乾燥處理用粉劑DS、水可分散的漿液處理用粉劑 ws、水溶性粉劑ss及乳液ES&amp;EC及凝膠調配物GF。該等 調配物可以稀釋或未稀釋形式施用至種子。可在播種前向 種子施用,其係直接施用至種子上或在使種子預萌芽後施 用。 在較佳實施例中,使用FS調配物進行種子處理。通常FS 調配物可包含1至800 g/1活性成份、!至2〇〇 g/i表面活性 劑、〇至200 g/Ι防凍劑、〇至4〇〇 g/丨黏合劑、〇至2〇〇 g/i顏 料及至多1升溶劑(水較佳)。 用於種子處理之式I或11化合物的其他較佳f s調配物包含 0.5-80 wt%活性成份、〇.〇5_5 wt%潤濕劑、〇5_15 wt% 分散 劑、0.1-5 wt%增稠劑' 5_20 wt%防凍劑' 〇」_2 wt%消泡 劑、1-20 wt%顏料及/或染料、〇_15 wt%黏著劑/黏合劑、 133661.doc -123 - 200917962 0-75 wt%填充劑/媒劑、以及o.w] .%防腐劑。 若適宜,可在即將使用前向活性成份中添加各種類型之 油、潤濕劑、佐劑、除草劑、殺真菌劑、其他殺蟲劑或殺 細菌劑(罐混合)。該等試劑通常以1:1〇至1〇:ι之重量比與 本發明試劑混合。 ' 式I或II化合物可經由接觸(經由土壤、玻璃、牆壁、蚊 帳、地毯、A物部分或動物部分)及攝食(誘飼或植物部分) 來生效。 隹用聆牴抗螞蟻、白蟻、黃蜂、蒼蠅、蚊子、蟋蟀… 蠊時,式I或II化合物較佳係以誘i耳組合物形式來使用。 誘I耳可為液體、固體或半固體製劑(例如凝膠)。固體誘 餌可形成適於各種應用之不同形狀與形式,例如顆粒、 塊、棒、盤。可將液體誘料充至各種裝置中以確保正確 施用’例如開口容器、噴濃裝置、液滴源或蒸發源。凝勝 可係基於水性或油性基質並可根據關於黏稠度、保渴性或 老化特性之具體需要來調配。 、〆 組合射所㈣㈣具有充分吸引力㈣誘諸如碼蟻、 :蟻、頁蜂、蒼蠅、蚊子、蟋蟀等昆蟲或斐蠊食用其之產 。可藉助攝食刺激劑或性外激素來操縱 激劑係非排哈性地@ έ &quot;, 5物刺 '、選自(例如)動物及/或植物蛋白(肉粉、 油y 、昆蟲部分、蛋黃)、動物及/或植物源脂肪及 油或早糖、寡糖或有機多綞,女、1益π 右旋糖、葡萄糖1粉=:::、乳糖、果糖、 物果膠或甚至糖蜜或蜂蜜。次耍、 作物、植物、動物、昆蟲之新鮮或腐觸部分或:二 13366] .doc •124· 200917962 亦可用作攝食刺激劑。已知性外激素具有更強昆蟲特異 性。具體外激素闡述於文獻中並已為熟習此項技術者所 知。 —乳浴膠(例如什W,丨厂/«7 -貝视物或幫浦噴灑物 形式之式I或II化合物之調配物非常適用於供非專業使用者 來控制諸如蠅類、蚤、蜱、蚊子或蜚蠊等害蟲。 乳 &gt;谷膠配 方較佳係由以下物質組成:活性化合物;溶劑, 合聞,例如低碳 醇(例如曱醇、乙醇、丙醇、丁醇)、_類(諸如丙_、曱基 乙基網)、沸點介於約50至250 t之間之石蠟烴(例如^ 油)、二甲基曱醯胺、N-甲基吡咯啶_、-田健π 一 T基亞砜、芳 香族烴(例如甲苯、二甲苯)、水;及一輔助劑,例如乳化 劑(例如山梨糖醇單油酸酯、具有3-7莫耳璜7 ^ 叩衣軋乙烷之油基 乙氧基化物、乙氧基化脂肪醇;芳香油(例如香精油)、中 碳腊肪酸與低碳醇之酯、芳香族羰基化合 υ σ物、(若適宜)穩 定劑(例如苯曱酸鈉)、兩性表面活性劑、 4 低妷環氧化物、 原甲酸三乙酯及(若需要)推進劑(例如丙烧、 J院、氮氣、 壓縮空氣、二甲謎、二氧化碳、氧化亞氮或該等氣體之ρ 合物)。 同 由於不使用推進劑,油性喷麗調配物與U㈣林 〇 式1或化合物及其各自組合物亦可用於蚊香及熏茱香、 熏煙匣、蒸發板或長效蒸發器中,H f … Μ T用於防虫主紙、防 虫主墊或其他不需加熱之蒸發器系統中。 &quot;式1或11化合物及其各自組合物來控制由昆蟲傳播之傳 133661.doc •125- 200917962 染性疾病(例如瘧疾、登革熱及黃熱病、淋巴性絲蟲病、 及利什曼病(leishmaniasis))之方法亦包含處理棚屋與房屋 表面、空氣噴灑及浸潰窗簾、帳篷、衣物、蚊帳、采采蠅 捕集器或諸如此類。施用至纖維製品、織物、針織品、非 織物、網狀材料或箔及防水油布之殺昆蟲組合物較佳包含 包括殺昆蟲劑、(視需要)防護劑及至少一種黏合劑之混合 物。舉例而言,適宜防護劑係N,N-二乙基-間-甲苯曱醯胺 (DEET)、N,N-二乙基苯基乙醯胺(DEpA)、卜^-環己小基_ 羰基)-2-甲基六氫吡啶、(2_羥曱基環己基)乙酸内酯、2_乙 基-1,3-己二醇、避蚊酮(indal〇ne)、曱基新癸醯胺 (MNDA)、不用於昆蟲控制之擬除蟲菊酯(例如{(+/_)_3_烯 丙基-2-甲基-4-氧代環戊_2-(+)_烯基_(+)_反_菊酸酯(賜百寧 (sbiothrin)))彳于自植物提取物或與植物提取物相同之防 護劑(如檸檬油精、丁香酚、( + )_Eucamal〇1⑴、㈠小表_ Eucamalol)、或得自以下植物之粗製植物提取物:如斑皮 桉(Eucalyptus maculata)、白背蔓荊(vitex r〇tundif〇lia)、 馬丁香(Cymb〇P〇gan martinii)、檸檬香茅(Cymb〇p〇gan cit慮S)(檸檬草)、香茅(Cym〇p〇gan 丽偷3) (ciu〇nella)。 舉例而έ ’適宜黏合劑係選自以下物質之聚合物與共聚 物·脂肪族酸之乙烯基酯(例如乙酸乙烯酯及柯赫酸乙烯 酯(vinyl versatate))、醇之丙烯酸酯及甲基丙烯酸酯(例如 丙烯酸丁酯、丙烯酸2-乙基己基酯、及丙烯酸曱酯)、單_ 及二乙烯系不飽和烴(例如苯乙烯)、及脂肪族二烯(例如丁 二烯)。 133661.doc • 126 - 200917962 簾文帳之/s: /貝通常係藉由將紡織品材料浸泡於式j 及π活性化合物之乳液或分散液中或將其喷灑至織物上 實施。 原則上,可用於處理種子之方法係業内已知之所有適宜 種子處理技術,且尤其係摔種技術,例如種子塗佈(例如 種子丸化)、藥粉拌種及種子吸脹(例如浸種)。 在本文中,&quot;種子處理&quot;係指使種子與式工或π化合物彼此 接觸之所有方法’且”拌種”係指向種子提m式⑽ 化合物之種子處理方法’即其產生包含式咖化合物之種 子。在原則上,可在種子收穫後至播種種子期間任何時間 對種子實施處理。可在即將種植種子之前或在種植種子期 間使用(例如)”播種箱”方法來處理種子。,然而,亦可在種 植種子之前若干周或若干個月(例如至多12個月)(例如)以 拌種處理形式實施處理’其中未觀察到效能大幅度降低。 可方便地對未播種種子實施處理。本文所用術語”未播 種種子&quot;意指包括自種子收穫至出於植物萌芽及生長目的 而將種子播種於土地中期間任一階段之種子。 具體而言,在處理中遵循一定程序,其中在適宜裝置 (例如用於混合固體或固/液配合物之混合裝置)中將種子與 期望置的未經處理的或預先用水稀釋之種子處理調配物混 合直至該組合物在種子上均勾分佈。若適宜,在此之後實 施乾燥步驟。 式I或II化合物或其對映異構體或獸醫學上可接受之鹽尤 其亦適合用於在動物體内及體表抵抗寄生蟲。 133661.doc •127- 200917962 因此,本發明另一目的係提供在動物體内及體表控制寄 生蟲之新方法。本發明另一目的係提供更安全之動物用殺 蟲劑。本發明另—目的係另外提供可以較現用殺蟲劑更低 T劑量使用之動物用殺蟲劑。且本發明另一目的係提供可 提供對寄生蟲長效殘留控制的動物用殺蟲劑。 本發明亦係關於含有殺寄生蟲有效量之式合物或 其對映異構體或獸醫學上可接受之鹽及可接受载劑之組合 物,其用於在動物體内及體表抵抗寄生蟲。 本發明亦提供處理、控制、預防及保護動物以抵抗寄生 轴侵擾及感木之方法,其包含向動物經口、局部或非經腸 投與或施用殺寄生蟲有效量之式I或Π化合物或其對映異構 體或獸醫學上可接受之鹽或包含其之組合物。 本發明亦提供製備用於處理、控制、預防或保護動物以 抵抗寄生蟲^擾或感染之組合物的方法,該組合物包含殺 寄生蟲有效量之式化合物或其對映異構體或獸醫學上 可接受之鹽或包含其之組合物。 化α物抵才几農業害蟲之活性不能說明其具有在動物體内 及體表控制内寄生蟲及外寄生蟲之適應性,例如該適應性 需要(在經口施用時)非催吐低劑量、與動物之代謝相容 性、低毒性、及操作安全性。 令人驚訴地,已發現式則化合物適用於在動物體内及 體表抵抗内寄生蟲及外寄生蟲。 式I或Π化合物或其對映異構體或獸醫學上可接受之鹽及 包含其之組合物較佳用於控制及預防對動物的侵擾:感 133661.doc -128- 200917962 染,包括溫血動物(包括人類)及魚類。舉例而言,其適用 於控制及預防對以下動物的侵擾及感染:哺乳動物,例如 牛、緯羊、豬、路騎、鹿、馬、小豬、家禽、兔、山羊、 犬及貓、水牛、驢、扁角鹿及馴鹿;亦及毛皮動物,例如 ^ 毛、’、糸乳及况瓶,鳥類,例如母雞、鶴、火雞及鴨; 及'、:、類例如淡水魚及咸水魚,例如鱒魚、經魚及鰻鱺。 式I或II化合物或其對映異構體或獸醫學上可接受之鹽及 包含其之組合物較佳用於控制及預防對家畜的侵擾及感 染,例如犬或貓。 溫血動物及魚類中之侵擾包括(但不限於)虱、羽虱' 蜱、鼻蠅、羊蜱蠅、叮咬飛蟲、蠅狀飛蟲、蠅類、蠅蛆幼 蟲、恙瞒、蚋、蚊及蚤。 式I或II化合物或其對映異構體或獸醫學上可接受之鹽及 包含其之組合物適用於全身性及/或非全身性控制外寄生 蟲及/或内寄生蟲。其可有效抵抗所有或某些發育階段。 式I或II化合物尤其可用於抵抗外寄生蟲。 、 式I或II化合物尤其可用於分別抵抗以下各目及各種之寄 生蟲· 蚤(蚤目(Siphonaptera)) ’ 例如貓櫛頭蚤(Cten〇cephalides felis)、犬褐頭蚤(Ctenocephalides canis)、印鼠客蚤 (Xenopsylla cheopis)、人蚤(puiex irritans)、穿皮潛蚤 (Tunga penetrans)、及具帶病蚤(Nosopsynus fasciatus), 蜚蠊(蜚蠊目(Blattaria-Blattodea)),例如德國小蠊、亞 洲小蠊(Blattella asahinae)、美洲大蠊(Peripianeta 133661.doc -129· 200917962 americana)、日本大蠊(Periplaneta japonica)、褐色大蠊 (Periplaneta brunnea)、黑胸大蠊(peripianeta fuligginosa)、 澳洲大蠊(Periplaneta australasiae)、及東方蜚蠊(Blatta orientalis), 蠅’蚊(雙翅目)’例如埃及伊蚊、白紋伊蚊(Aedes albopictus)、刺擾伊蚊、墨西哥橘實蠅、五斑按蚊、災難 按蚊(Anopheles crucians)、白魔按蚊(Anopheles albimanus)、岡比亞按蚊(Anopheles gambiae)、弗裏伯恩 氏按蚊(Anopheles freeborni)、白騍按蚊(Anopheles leucosphyrus)、微小按蚊(Anopheles mini-mus)、四斑按蚊 (Anopheles quadrimaculatus)、紅頭麗蠅(Calliphora vicina)、蛆症金蠅、螺旋金蠅、肉旋金蠅、中室斑虻 (Chrysops discalis)、靜斑虻(Chrysops silacea)、大西洋斑 虻(Chrysops atlanticus)、嗜人錐蠅(Cochliomyia hominivorax)、嗜人瘤蠅、毛庫蠓(Culicoides furens)、五 帶淡色庫蚊、魏仙庫蚊(Culex nigripalpus)、致倦庫蚊 (Culex quinquefasciatus)、附斑庫蚊(Culex tarsalis)、填蚊 (Culiseta inornata)、黑尾脈毛蚊(Culiseta melanura)、人皮 繩(Dermatobia hominis)、黃腹廄蠅、大馬胃蠅、采采蠅、 須舌繩(Glossina palpalis)、引舌繩(Glossina fuscipes)、膠 舌繩(Glossina tachinoides)、騷擾角绳、鞍癭癭蚊、潛繩 屬(Hippelates spp·)、蚊皮蠅、托倫斯細蠓(Lep-toconops torrens)、羊綠蠅、銅綠蠅、絲光綠蠅、玉頸洛克绳、曼 蚊屬(Mansonia spp.)、家繩、廄腐罐、羊鼻蠅、銀足白蛉 133661.doc -130- 200917962 (Phlebotomus ar-gentipes)、哥倫比亞鱗蚊(psor〇ph〇ra columbiae)、變色鱗蚊(Psorophora discolor)、梅克斯特原 蚋(Prosimulium mixtum)、赤尾麻蠅(Sar-cophaga haemorrhoidalis)、麻繩屬(Sarcophaga sp ·)、帶納 (Simulium vittatum)、廄螫蠅(Stomoxys calcitrans)、牛 虻、北美黑虻(Tabanus atratus)、細線原虻(Tabanus lineola)、及擬原 it(Tabanus similis), 虱(虱毛目(Phthiraptera)),例如頭蝨(pediculus humanus capitis)、體風(Pediculus humanus corporis)、和陰風 (Pthirus pubis)、牛血風(Haematopinus eurysternus)、豬 jk 風(Haematopinus suis)、牛顆風(Linognathus vituli),牛毛 風(Bovicola bovis)、雞短角羽風(Menopon gallinae)、雞體 虱(Menacanthus stramineus) ' 及水牛盲虱(Solenopotes capillatus), 碑及寄生性蜗(寄瞒目(Parasitiformes)):蜱(蜱亞目 (Ixodida)),例如肩突硬蜱(lx〇des scapularis)、全環硬碑 (Ixodes holocyclus)、太平洋硬蜱(Ixodes pacificus)、jk 紅 扇頭蜱(Rhiphicephalus sanguineus)、安德遜氏革蜱 (Dermacentor andersoni)、變異革碑(Dermacentor variabilis)、美洲花蜱、盲壁風(Ambryomma maculatum)、 赫莫斯軟碑(Ornithodorus hermsi)、回歸熱蜱(Ornithodoros turicata)及寄生性蜗(中氣門亞目(Mesostigmata)),例如熱 帶鼠恙蟲(Orni-thonyssus bacoti)及雞皮刺蜗, 輻蜗亞目(Actinedida)(氣門亞目(Prostigmata))及粉蜗亞 133661.doc -131 - 200917962 目(Acaridida)(無氣門亞目(Astigmata))例如蟎屬(Acarapis spp.)、姬螯蜗屬(Cheyletiella spp.)、禽螯蜗屬 (Ornithocheyletia spp.)、肉蟎屬(Myobia spp.)、瘡蝠屬 (Psorergates spp.)、脂瞒屬(Demodex spp.)、恙蜗屬 (Trombicula spp.)、凸奪蜗屬(Listrophorus spp.)、壁風 (Acarus spp.) ' 食路蜗屬(Tyrophagus spp.)、嗜木蜗屬 (Caloglyphus spp.)、低戴克蟎屬(Hyp〇dectes spp.)、翅蝶 屬(Pterolichus spp_)、癢蟎屬(Psoroptes spp·)、皮蟎屬 ( (Chorioptes spp.)、耳癢蟎屬(〇t〇dectes spp.)、疥蟎屬 (Sarcoptes spp.)、耳瞒屬(Notoedres spp.)、鳥疮蜗屬 (Knemidocoptes spp.)、胞蟎屬(cytodites spp.)、及雞離蟎 屬(Laminosioptes spp.), 臭蟲(異翅亞目(Heteropterida)):溫帶臭蟲(Cimex lectularius)、熱帶臭蟲(Cimex hemipterus)、白頭撒堵 (Reduvius senilis)、錐撒蝽屬(Triatoma spp.)、紅獵蝽屬 (Triatoma spp·)、錐蝽屬(Panstrongylus ssp_)及輪蝽(Arilus 、. critatus), 乳目(Anoplurida) ’ 例如血風屬(Haematopinus spp·)、長 顎風屬(Linognathus spp.)、星屬(pediculus spp.)、陰風屬 (Phtirus spp.)及盲風屬(Solenopotes spp.), 食毛目(Mallophagida)(亞目 Amblycerina 及 Ischnocerina), 例如毛鳥虱(Trimenopon spp·)、禽虱屬(Menopon spp.)、鴨 虱屬(Trinoton spp·)、牛羽虱屬(Bovicola spp.)、韋耐虱屬 (Werneckiella spp,)、萊皮虱屬(Lepikentron spp,)、齧毛虱 133661.doc -132- 200917962 屬(Trichodectes spp.)及貓毛虱屬(Felicola spp.), 虫回蟲線蟲綱(Roundworms Nematoda): 犬鞭蟲(Wipeworms)及旋毛蟲(Trichinosis)(毛管目 (Trichosyringida)),例如毛線蟲科(Trichinellidae)(毛線蟲 屬(Trichinella spp.))、(鞭蟲科(Trichuridae))鞭蟲屬 (Trichuris spp.)、毛細線蟲屬(Capillaria spp.), 桿線蟲(Rhabditida),例如小桿線蟲屬(Rhabditis spp.)、 類圓線蟲屬(Strongyloides spp.)、海賴斯線蟲屬 (Helicephalobus spp.), 圓線蟲目(Strongylida),例如圓線蟲屬(Strongylus spp.)、鈎口 線蟲屬(Ancylostoma spp.)、美洲鈎蟲(Necator americanus)、仰口 線蟲屬(Bunosto-mum spp.)(釣蟲 (Hookworm))、毛管線蟲屬(Trichostrongylus spp.)、撚轉 血矛線蟲(Haemonchus contortus)、奥斯特他氏線蟲屬 (Ostertagia spp.)、古柏線蟲屬(Cooperia spp.)、細頸線蟲 屬(Nematodirus spp.)、網尾線蟲屬(Dictyocaulus spp.)、盅 口 線蟲屬(Cyathostoma spp.)、 結節線蟲屬 (Oesophagostomum spp.)、牙冠線蟲(Stephanurus dentatus)、沃魯線蟲屬(OUulanus spp.)、夏氏線蟲屬 (Chabertia spp.)、氣管比翼線蟲(Syngamus trachea)、鈎蟲 屬(Uncinaria spp.)、球頭線蟲屬(Globocephalus spp·)、板 口 線蟲屬(Necator spp.)、後圓線蟲屬(Metastrongylus spp.)、毛細缪勒線蟲(Muellerius capillaris)、原圓線蟲屬 (Protostrongylus spp.)、血管圓線蟲屬(Angiostrongylus 133661.doc -133 - 200917962 SPP·)、擬馬鹿圓線蟲屬(Parelaphostrongylus spp.)、奥妙薄苗 圓線蟲(Aleurostrongylus abstrusus)、及腎膨結線蟲 (Dioctophyma renale) » 蛔蟲(Intestinal roundworms)(蛔蟲目(Ascaridida)),例如 人蛔蟲(Ascaris lumbricoides)、豬蛔蟲(Ascaris suum)、雞 細蟲(Ascaridia galli)、馬细蟲(Parascaris equorum)、蟯蟲 (Enterobius vermicularis)(細長線蟲(Threadworm))、犬弓 蛔蟲(Toxocara canis)、獅弓蛔線蟲(Toxascaris leonine)、 '' 斯克裏亞賓線蟲屬(Skrjabinema spp.)、及馬尖尾線蟲 (Oxyuris equi), 駝形目(Camallanida),例如麥地那龍線蟲(Dracunculus medinensis) (guinea worm), 旋尾目(Spirurida),例如吸吮線蟲屬(Thelazia spp.)、吳 策線蟲屬(Wuchereria spp.)、布魯斯蟲屬(Brugia spp.)、盤 尾線蟲屬(Onchocerca spp·)、惡絲蟲屬 9Dirofilari spp.)、 棘唇線蟲屬(Dipetalonema spp.)、腹腔絲蟲屬(Setaria .·: ' spp.)、企管絲蟲屬(Elaeophora spp.)、盧氏尾旋線蟲 (Spirocerca lupi)、及麗線蟲屬(Hab -ronema spp.) » 棘頭蟲 (Thorny headed worms)( 棘頭蟲綱 (Acanthocephala)) ’ 例如棘頭蟲屬(Acanthocephalus SPP·)、豬 巨 吻棘頭 蟲(Macrae an thorhynchus hirudinaceus)、及釣棘頭蟲屬(〇ncic〇ia spp.), 滿蟲(Planarians)(扁形動物門(Plathelminthes)): 吸蟲(Flukes)(吸蟲綱(Trematoda)),例如片吸蟲屬 133661.doc -134- 200917962 (Faciola spp.)、大擬片吸蟲(Fascioloides magna)、並殖吸 蟲屬(Paragonimus spp.)、雙腔吸蟲屬(Dicrocoelium spp.)、布氏薑片吸蟲(Fasciolopsis buski)、華支睾吸蟲 (Clonorchis sinensis)、裂體吸蟲屬(Schistosoma spp.)、毛 血吸蟲屬(Trichobilharzia spp.)、有翼重翼吸蟲(Alaria alata)、並殖吸蟲屬(Paragonimus spp.)、及諾赛特吸蟲屬 (Nanocyetes spp.), 海扁蟲(Cercomeromorpha),尤其多節縧蟲亞綱 (Cestoda)(、條蟲(Tapeworms)), 例如裂頭縧蟲屬 (Diphyllobothrium spp.)、帶縧蟲屬(Tenia spp·)、棘球縧蟲 屬(Echinococcus spp.)、犬複殖孔縧蟲(Dipylidium caninum)、多頭縧蟲屬(Multiceps spp.)、膜殼縧蟲屬 (Hymenolepis spp.)、卞殖孔鄉蟲屬(Mesocestoides spp·)、 蝙蝠皮縧蟲屬(Vampirolepis spp.)、蒙尼茨縧蟲屬 (Moniezia spp.)、裸頭縧蟲屬(Anoplocephala spp.)、叠宮 縧蟲屬(Sirometra spp·)、裸頭縧蟲屬(Anopi〇cephala spp.)、及膜殼縧蟲屬(Hymenolepis spp.), 式I或II化合物及包含其之組合物尤其可用於控制雙翅 目、蚤目及蜱亞目之害蟲。 此外,式I或II化合物及包含其之組合物用於抵抗蚊子之 用途尤佳。 本發明另一較佳實施例係式1或II化合物及包含其之組合 物用於抵抗蠅類之用途。 此外,式I或II化合物及包含其之組合物用於抵抗蛋類之 133661.doc •135· 200917962 用途尤佳。 本發明另—較佳實施例係式I或π化合物及包含其之組合 物用於抵抗蜱類之用途。 式I或II化合物及包含其之組人 ',且σ物亦尤其可用於抵抗内寄 生蟲(細蟲線蟲、棘頭蟲及渦蟲)。 可以預防性及治療性方式實施投與。 活性化合物之投與係直接或以適宜製劑形式以經口、局 部/經皮或非經腸方式來實施。G) Water-dispersible powder and water-soluble powder (WP, SP, SS, WS) 75 parts by weight of the active compound were ground in a rotor-precipitator mill by adding 25 parts by weight of a dispersant, a wetting agent and silicone. A stable dispersion or solution of the active compound is obtained by diluting with water, whereby a formulation containing an active compound of 75 ° (w/w) is obtained. H) gel formulation (GF) in agitating ball mill, adding 1 part by weight of dispersant, 1 part by weight of agglomerating agent (5) wet agent and 70 parts by weight of water or organic solvent, 2 parts by weight The number of active compounds is comminuted to obtain a fine suspension of the active compound. Dilution with water gives a stable suspension of the active compound, whereby a formulation containing 20% (w/w) of active compound is obtained. 2. For the application of leaf application without dilution. For seed treatment, the products may be applied to the seed in a diluted or undiluted form. U-sprayable powder (DP, DS) 5 parts by weight of activated human extracts, ground, and thoroughly mixed with 95 parts by weight of refined mulch. Thus, 133661, doc-122·200917962 J) granules (GR, FG, GG, MG) of the active compound having a W (Ww) activity are obtained, and 0.5 parts by weight of the active compound are finely ground and 95 parts by weight The carrier 1J was mixed 'by this to obtain a formulation containing 0.5% (w/w) of the active compound. Current methods are extrusion, spray drying or fluidized beds. This results in particles that are used in blade applications without dilution. K) ULV solution (UL) 10 parts by weight of the active compound are dissolved in 9 parts by weight of an organic solvent such as xylene. This gives a product containing 1% (w/w) of active compound which can be used for blade application without dilution. Compounds of formula II or II are also suitable for the treatment of plant propagation material (eg seeds). Conventional seed treatment formulations include, for example, flowable concentrate FS, solution LS, dry treatment powder DS, water dispersible slurry treatment powder ws, water soluble powder ss and emulsion ES&amp;EC and gel formulation GF . The formulations can be applied to the seed in diluted or undiluted form. Seeds can be applied prior to sowing, either directly to the seed or after pre-emergence of the seed. In a preferred embodiment, the FS formulation is used for seed treatment. Usually FS formulations can contain from 1 to 800 g/1 active ingredient! Up to 2〇〇g/i surfactant, 〇 to 200 g/Ι antifreeze, 〇 to 4〇〇g/丨 binder, 〇 to 2〇〇g/i pigment and up to 1 liter of solvent (water is preferred) . Other preferred fs formulations of the compound of formula I or 11 for seed treatment comprise from 0.5 to 80% by weight of active ingredient, 〇.〇5_5 wt% wetting agent, 〇5_15 wt% dispersant, 0.1-5 wt% thickening Agent '5_20 wt% antifreeze' 〇"_2 wt% defoamer, 1-20 wt% pigment and / or dye, 〇 _ 15 wt% adhesive / binder, 133661.doc -123 - 200917962 0-75 wt % filler/vehicle, and ow].% preservative. If appropriate, various types of oils, wetting agents, adjuvants, herbicides, fungicides, other insecticides or bactericides (tank mix) may be added to the active ingredient just prior to use. These agents are usually mixed with the reagent of the present invention in a weight ratio of 1:1 Torr to 1 Torr. Compounds of formula I or II may be effective by contact (via soil, glass, walls, mosquito nets, carpets, part A or animal parts) and ingestion (feeding or plant parts). When the cockroach is used against ants, termites, wasps, flies, mosquitoes, cockroaches, cockroaches, the compound of formula I or II is preferably used in the form of a stimulating composition. The mutin can be a liquid, solid or semi-solid preparation (e.g., a gel). Solid baits can be formed into different shapes and forms suitable for a variety of applications, such as granules, blocks, rods, trays. Liquid lures can be charged into various devices to ensure proper application 'e.g., open containers, spray devices, droplet sources, or evaporation sources. Condensation can be based on aqueous or oily matrices and can be formulated according to the specific needs of the viscosity, thirst retention or aging characteristics. 〆 Combination shots (4) (4) Fully attractive (4) Inducing insects such as code ants, ants, page bees, flies, mosquitoes, cockroaches, or Fischers. The stimulant or sexual pheromone can be used to manipulate the non-exclusive genus @ έ &quot;, 5 thorns, selected from, for example, animal and/or vegetable proteins (meat, oil y, insect parts, egg yolk) ), animal and / or plant derived fats and oils or early sugar, oligosaccharides or organic polysaccharides, female, 1 π dextrose, glucose 1 powder =:::, lactose, fructose, pectin or even molasses or honey. Secondary, crop, plant, animal, insect fresh or rotted parts or: 2 13366] .doc •124· 200917962 Can also be used as a food stimulant. Sex hormones are known to have greater insect specificity. Specific pheromones are described in the literature and are known to those skilled in the art. - milk bath gel (for example, the formulation of the compound of formula I or II in the form of WW, 丨厂/«7 -beixiang or pump spray is very suitable for non-professional users to control such as fly, cockroach, cockroach , pests such as mosquitoes or cockroaches. Milk &gt; gluten formula is preferably composed of the following substances: active compound; solvent, sensible, such as lower alcohol (eg sterol, ethanol, propanol, butanol), _ class (such as C-, mercaptoethyl network), paraffin hydrocarbons (such as ^ oil) with a boiling point between about 50 and 250 t, dimethyl decylamine, N-methyl pyrrolidine _, - Tian Jian π a T-based sulfoxide, an aromatic hydrocarbon (such as toluene, xylene), water; and an adjuvant, such as an emulsifier (such as sorbitol monooleate, having 3-7 moles 7 ^ 轧An oil-based ethoxylate, an ethoxylated fatty alcohol; an aromatic oil (such as an essential oil), an ester of a medium-carbon fatty acid and a lower alcohol, an aromatic carbonyl compound σ σ, (if appropriate) a stabilizer (eg sodium benzoate), amphoteric surfactant, 4 low oxime epoxide, triethyl orthoformate and, if necessary, propellant ( For example, C-burn, J hospital, nitrogen, compressed air, dimethyl mystery, carbon dioxide, nitrous oxide or ρ of these gases.) Also because of the use of propellant, oily spray formulation and U (four) forest 〇 1 or The compounds and their respective compositions can also be used in mosquito coils and smoked musk, fumigation, evaporation boards or long-acting evaporators, H f ... Μ T for insect-resistant main paper, insect-resistant main mat or other evaporators without heating In the system. &quot;Formula 1 or 11 compounds and their respective compositions to control transmission by insects 133661.doc •125- 200917962 Sexually transmitted diseases (eg malaria, dengue and yellow fever, lymphatic filariasis, and leish The method of leishmaniasis also includes the treatment of sheds and house surfaces, air spraying and dipping curtains, tents, clothing, mosquito nets, tsetse traps or the like. Applied to fabrics, fabrics, knitwear, non- The insecticidal composition of the fabric, mesh material or foil and tarpaulin preferably comprises a mixture comprising an insecticide, (as needed) a protective agent and at least one binder. For example, a suitable protective agent N, N-Diethyl-m-toluidine (DEET), N,N-diethylphenylacetamide (DEpA), ^-cyclohexyl _ carbonyl)-2-methylhexahydropyridine , (2-hydroxydecylcyclohexyl)acetic acid lactone, 2-ethyl-1,3-hexanediol, indole oxime, decyl neodecylamine (MNDA), not used for insect control Pyrethroids (eg, {(+/_)_3_allyl-2-methyl-4-oxocyclopenta-2-(+)-alkenyl-(+)-trans-chrysanthemate (sbiothrin)) from plant extracts or the same protective agents as plant extracts (such as lemon olein, eugenol, ( + ) _Eucamal 〇 1 (1), (a) small table _ Eucamalol), or derived from Crude plant extracts of the following plants: Eucalyptus maculata, vitex r〇tundif〇lia, Cymb〇P〇gan martinii, Lemongrass (Cymb〇p〇gan) Cit considers S) (lemon grass), lemongrass (Cym〇p〇gan 丽 steal 3) (ciu〇nella). For example, 'suitable binders are selected from the group consisting of polymers and copolymers of the following materials: vinyl esters of aliphatic acids (such as vinyl acetate and vinyl versatate), acrylates of alcohols and methyl groups. Acrylates (e.g., butyl acrylate, 2-ethylhexyl acrylate, and decyl acrylate), mono- and diethylene-based unsaturated hydrocarbons (e.g., styrene), and aliphatic diolefins (e.g., butadiene). 133661.doc • 126 - 200917962 Curtain / s: / shell is usually carried out by soaking the textile material in an emulsion or dispersion of the formula j and π active compound or spraying it onto the fabric. In principle, the methods which can be used to treat seeds are all suitable seed treatment techniques known in the art, and in particular, techniques for seeding, such as seed coating (e.g., seed pelleting), powder dressing, and seed swelling (e.g., seed soaking). In this context, &quot;seed treatment&quot; refers to all methods of making seeds and formula or π compounds in contact with each other 'and' seed dressings are directed to the seed treatment method of the formula (10) compound, ie, the production of the inclusion compound compound Seeds. In principle, the seed can be treated at any time after seed harvesting until seeding. Seeds can be treated using, for example, a "sowbox" method prior to planting the seed or during planting the seed. However, it is also possible to carry out the treatment in the form of seed dressing for several weeks or several months (e.g., up to 12 months) before planting the seed' where no significant decrease in potency is observed. Untreated seeds can be conveniently treated. The term "unseeded seeds" as used herein, is meant to include seeds that are harvested from seed to seed at any stage during the germination and growth of the plant for the purpose of plant germination. In particular, certain procedures are followed in the treatment, A suitable device, such as a mixing device for mixing solid or solid/liquid complexes, is mixed with the desired untreated or pre-water diluted seed treatment formulation until the composition is Hooked on the seed. If appropriate, the drying step is carried out afterwards. The compounds of the formula I or II or their enantiomers or veterinary acceptable salts are also especially suitable for combating parasites in and on animals. 133661.doc • 127- 200917962 Accordingly, another object of the present invention is to provide a novel method of controlling parasites in and on animals. Another object of the present invention is to provide a safer insecticide for animals. An animal insecticide that can be used at a lower T dose than the current insecticide. Another object of the present invention is to provide an animal that can provide long-lasting control of parasites. The invention also relates to a composition comprising a parasiticidally effective amount of a compound or an enantiomer or a veterinarily acceptable salt thereof and an acceptable carrier for use in an animal The body surface is resistant to parasites. The invention also provides a method for treating, controlling, preventing and protecting an animal against parasitic axis infestation and sensation, comprising administering to the animal an oral, topical or parenteral administration or application of a parasiticidally effective amount. Formula I or a guanidine compound or an enantiomer or veterinary acceptable salt thereof or a composition comprising the same. The invention also provides for the preparation, treatment, control, prevention or protection of an animal against parasites or A method of infecting a composition comprising a parasiticidally effective amount of a compound of the formula or an enantiomer or a veterinary acceptable salt thereof or a composition comprising the same. The activity does not indicate that it has the adaptability of endoparasites and ectoparasites in the body and on the surface of the body, such as the need for adaptation (at the time of oral administration), low dose of non-emetic, metabolic compatibility with animals, low toxicity, Operational safety. Incidentally, it has been found that the compounds are suitable for combating endoparasites and ectoparasites in and on animals. Formula I or hydrazine compounds or their enantiomers or veterinary The accepted salt and the compositions comprising the same are preferably used for controlling and preventing infestation to animals: Sense 133661.doc -128- 200917962 Dyeing, including warm-blooded animals (including humans) and fish. For example, it is suitable for control And prevention of infestation and infection of the following animals: mammals such as cattle, latitude sheep, pigs, road riders, deer, horses, piglets, poultry, rabbits, goats, dogs and cats, buffalo, donkeys, flat-horned deer and reindeer; And fur animals such as hair, ', milk and bottle, birds, such as hens, cranes, turkeys and ducks; and ', :, such as freshwater fish and saltwater fish, such as squid, fish and oysters The compound of formula I or II, or an enantiomer or veterinary acceptable salt thereof, and compositions comprising the same are preferably used to control and prevent infestation and infection to livestock, such as dogs or cats. Infestations in warm-blooded animals and fish include (but are not limited to) cockroaches, cockroaches, cockroaches, larvae, larvae, biting worms, fly-like worms, flies, larvae, cockroaches, cockroaches, cockroaches And 蚤. The compound of formula I or II, or an enantiomer or veterinary acceptable salt thereof, and compositions comprising the same are suitable for systemic and/or non-systemic control of ectoparasites and/or endoparasites. It is effective against all or some stages of development. The compounds of formula I or II are especially useful against ectoparasites. The compounds of formula I or II are especially useful for combating the following and various parasites (Siphonaptera), such as Cten〇cephalides felis, Ctenocephalides canis, Xenopsylla cheopis, puiex irritans, Tunga penetrans, and Nosopsynus fasciatus, Blattaria-Blattodea, such as Germany Small cockroach, Asian cockroach (Blattella asahinae), American cockroach (Peripianeta 133661.doc -129· 200917962 americana), Japanese giant cockroach (Periplaneta japonica), brown cockroach (Periplaneta brunnea), black-breasted cockroach (peripianeta fuligginosa) , Periplaneta australasiae, and Blatta orientalis, fly 'Diptera (Diptera)' such as Aedes aegypti, Aedes albopictus, Aedes aegypti, Mexican orange fly , Anopheles sinensis, Anopheles crucians, Anopheles albimanus, Anopheles gambiae, Anophe Eles freeborni), Anopheles leucosphyrus, Anopheles mini-mus, Anopheles quadrimaculatus, Calliphora vicina, cockroach fly, spiral gold fly, meat Chrysops discalis, Chrysops silacea, Chrysops atlanticus, Cochliomyia hominivorax, Tumor flies, Culicoides furens Culex pipiens pallens, Culex nigripalpus, Culex quinquefasciatus, Culex tarsalis, Culiseta inornata, Culiseta melanura, human Dermatobia hominis, yellow-bellied scorpion fly, squid, tsetse fly, Glossina palpalis, Glossina fuscipes, Glossina tachinoides, harassment horn, saddle瘿瘿 mosquitoes, Hippelates spp·, mosquito flies, Lep-toconops torrens, sheep green fly, pheasant fly, silky green fly, jade neck rope, Mandonia Spp.) House rope, carrion can, sheep nose, silver foot white 133661.doc -130- 200917962 (Phlebotomus ar-gentipes), Colombian scale mosquito (psor〇ph〇ra columbiae), color-changing mosquito (Psorophora discolor), plum Prosimulium mixtum, Sar-cophaga haemorrhoidalis, Sarcophaga sp., Simulium vittatum, Stomoxys calcitrans, Burdock, North American blackbird (Tabanus) Atratus), Tabanus lineola, and Tabanus similis, Phthiraptera, such as pediculus humanus capitis, Pediculus humanus corporis, and yin Pthirus pubis), Haematopinus eurysternus, Haematopinus suis, Linognathus vituli, Bovicola bovis, Menopon gallinae, Menacanthus Stramineus) ' and Solenopotes capillatus, monument and parasitic worm (Parasitiformes): 蜱 (Ixodida), such as the shoulder torsion (lx〇de s scapularis), Ixodes holocyclus, Ixodes pacificus, JH Rhiphicephalus sanguineus, Dermacentor andersoni, Dermacentor variabilis, American bud, Ambryomma maculatum, Ornithodorus hermsi, Ornithodoros turicata, and parasitic worm (Mesostigmata), such as the tropical locust (Orni) -thonyssus bacoti) and chicken skin snail, Actinedida (Prostigmata) and powder worm 133661.doc -131 - 200917962 (Acaridida) (Astigmata) such as 螨Genus (Acarapis spp.), Cheyletiella spp., Ornithocheyletia spp., Myobia spp., Psorergates spp., Demodex Spp.), Trombula spp., Listrophorus spp., Acarus spp. 'Tyrophagus spp., Caloglyphus spp. , low dynasty (Hyp〇dectes spp.) Pterolichus spp_, Psoroptes spp., Chorioptes spp., 〇t〇dectes spp., Sarcoptes spp., ear Notoedres spp., Knemidocoptes spp., cytodites spp., and Laminosioptes spp., bedbug (Heteropterida): temperate zone Bedbug (Cimex lectularius), tropical bug (Cimex hemipterus), Reduvius senilis, Triatoma spp., Triatoma spp., Panstrongylus ssp_ and round A (Arilus, . critatus), Anoplurida ' For example, Haematopinus spp., Linognathus spp., pediculus spp., Phtirus spp. Solenopotes spp., Mallophagida (Amblycerina and Ischnocerina), such as Trimenopon spp., Menopon spp., Trinoton spp. , Bovicola spp., Werneckiella spp, Lepikentron spp, 133661.doc -132- 200917962 genus (Trichodectes spp.) and genus Felicola spp., Roundworms Nematoda: Wipeworms And Trichinosis (Trichosyringida), such as Trichinellidae (Trichinella spp.), Trichuridae (Trichuris spp.), Capillaria spp., Rhabditida, such as Rhabditis spp., Strongyloides spp., Helicephalobus spp., A. elegans (Strongylida), for example, Strongylus spp., Ancylostoma spp., Necator americanus, Bunosto-mum spp. (Hookworm), Trichostrongylus spp., Haemonchus contortus, Ostertagia spp., Cooperia spp., Nematodirus spp. ), net tail line Dictyocaulus spp., Cyathostoma spp., Oesophagostomum spp., Stephanurus dentatus, OUulanus spp., Chastera Chabertia spp.), Syngamus trachea, Uncinaria spp., Globocephalus spp., Necator spp., Metastrongylus spp. , Muellerius capillaris, Protostrongylus spp., A. elegans (Angiostrongylus 133661.doc -133 - 200917962 SPP·), Parelaphostrongylus spp., Omega Aleurostrongylus abstrusus and Dioctophyma renale » Intestinal roundworms (Ascaridida), such as Ascaris lumbricoides, Ascaris suum, chicken worms Ascaridia galli), Parascaris equorum, Enterobius vermicularis (Threadworm), Toxoplasma gondii (Tox Ocara canis), Toxascaris leonine, ''Skrjabinema spp.'), and Oxyuris equi, Camallanida, such as Dracunculiasis (Dracunculus medinensis) (guinea worm), Spirurida, such as Thelazia spp., Wuchereria spp., Brugia spp., Onchocerca Spp·), 9Dirofilari spp.), Dipetalonema spp., Setaria .·: ' spp., Elaeophora spp., Lushi tail Helicobacter species (Spirocerca lupi) and Hab-ronema spp. » Thorny headed worms (Acanthocephala) such as Acanthocephalus SPP·, pig giant Machae an thorhynchus hirudinaceus, and 〇ncic〇ia spp., Planarians (Plathelminthes): Flukes (Fagidae) Trematoda)), for example, flukes 133661.doc -134 - 200917962 (Faciola spp.), Fascioloides magna, Paragonimus spp., Dicrocoelium spp., Fasciolopsis buski , Clonorchis sinensis, Schistosoma spp., Trichobilharzia spp., Alaria alata, Paragonimus spp .), and Nanocyetes spp., Cercomeromorpha, especially Cestoda (Tapeworms), such as Diphyllobothrium spp. ), Tenia spp., Echinococcus spp., Dipylidium caninum, Multiceps spp., Hymenolepis spp. Mesocestoides spp., Vampirolepis spp., Moniezia spp., Anoplocephala spp., Sirometra spp ·), Anopi〇cephala spp., And the genus Hymenolepis spp., the compound of formula I or II and compositions comprising the same are particularly useful for controlling pests of the order Diptera, Acarina and Sphaerocephala. Furthermore, the compounds of formula I or II and compositions comprising the same are particularly useful for combating mosquitoes. Another preferred embodiment of the invention is a compound of formula 1 or II and compositions comprising the same for use in combating flies. In addition, the compounds of formula I or II and compositions comprising the same are particularly useful for combating eggs 133661.doc • 135. 200917962. Another preferred embodiment of the invention is a compound of formula I or π and a composition comprising the same for use in combating mites. The compound of formula I or II and the group comprising the same, and the sigma is also particularly useful for combating endogenous insects (microbes, echinoderms and planarians). Administration can be implemented in a prophylactic and therapeutic manner. Administration of the active compound is carried out in an oral, topical/transdermal or parenteral manner, either directly or in a suitable formulation.

對於經口投與溫血動物,可將4 I七了 Τ儿人 j將式I或II化合物調配為動物 飼料、動物飼料預混合料、動物飼料滚縮物、丸劑、溶 液、膏劑、懸浮液、獸用頓服藥、凝膠、㈣卜大丸劑及 膠囊。另外,式I或π化合物可以存於飲用水中之方式投| 動物。對於口服投與’所選劑型應向動物提供0.01 mg/kg 至⑽叫⑽動物體重/天之式工或„化合物,較佳以05 mg/kg至100 mg/kg動物體重/天提供。 或者’可以非經腸方式(例如藉由瘤胃内、肌内、靜脈 内或皮下注射)將式邮化合物投與動物。可將式則化 合物分散或溶解於生理學上可接受之之載劑中以供皮下注 射。或者’可將式【或η化合物調配為植入物以供皮下投 與。此外,可將式邮化合物經皮投與動物。對於非經腸 投與’所選劑型應向動物提供0.01叫心至1〇〇以心動物 體重/天之式1或II化合物。 亦可以 劑、粉末 以下形式將式I或II化合物局部施用至動物:浸 、粉劑、爱員圈、圓飾物、噴麗劑、洗髮劑、點施 133661 .doc -136· 200917962 及注把S周配物、及軟膏或水包油或油包水乳液。對於局部 施用,浸劑及噴灑劑通常含有0.5 ppm至5 〇〇〇 ppm且較佳i ppm至3 000 ppm之式化合物。此外,可將式化合 物調配成動物(尤其諸如牛及綿羊等四足動物)耳標。 適宜製劑係: 溶液,例如口服溶液、稀釋後口服投與之濃縮物、用於 皮膚上或體腔内之溶液、注施調配物、凝膠; 口服或經皮投與之乳液及懸浮液;半固體製劑; 其中以軟膏基或水包油或油包水乳液基加工活性化合物 之調配物; 固體製劑,例如粉劑、預混合物或濃縮物、顆粒、片 劑、錠劑、大丸劑、膠囊;煙霧劑及吸入劑、及含有活性 化合物之成形物品。 適於注射之組合物係藉由將活性成分溶解於適宜溶劑 中’並視需要添加諸如酸、鹼、緩衝鹽、防腐劑、及增溶 劑等其他成份來製備。對溶液實施無菌過濾及填充。 適宜溶劑係生理學上可耐受溶劑,例如水、烷醇,例如 乙醇、丁醇、笨甲醇、甘油、丙二醇、聚乙二醇、Ν_甲基 吡咯啶酮、2-吡咯啶酮、及其混合物。 可視需要將活性化合物溶解於生理學上可耐受的適於注 射的植物油或合成油中。 適且增办劑係可促進活性化合物在主溶劑中溶解或防止 其沈澱之’合劑。實例係聚乙烯吡咯啶酮、《乙烯醇、聚氧 乙基化蓖麻油、及聚氧乙基化山梨醇酐酯。 133661.doc -137- 200917962 適且防腐劑係苯甲醇 _ ιΤ 本τ和二虱丁酵、對羥基苯甲酸酯、及 此丁醇。 :服溶液係直接投與。在預先稀釋至使用濃度後經口投 、%物° 口服溶液及濃縮物係根據當前技術及如上文針 溶液所述方法來製備,消毒過程不係必需。 用於皮膚上之溶液传祐潘 從你被滴上、塗上、擦入、灑上或噴 上0 、用於皮膚上之溶液係根據當前技術及如上文針對注射溶 液所述方法來製備,消毒過程不係必需。 其他適宜溶劑係聚丙二醇、苯基乙醇、苯氧基乙醇、酯 (例如乙酸乙s旨或乙酸丁®旨、苯甲酸f基s旨)、_類(例如伸 •元基一醇烷基醚’例如二丙二醇單甲醚)、酮類(例如丙 酮、甲基乙基酮)、芳香族烴、植物油及合成油、二甲基 甲醯胺、二甲基乙酿胺、乙二醇單乙_一叫、丙嗣 縮甘油(solkeul)、碳酸丙二酯、及其混合物。 \ 在製備期間較佳可添加增_ ^適宜增㈣係:無機增 稠劑’例如膨潤土、膠質矽酸、單硬脂酸鋁;有機增二 劑,例如纖維素衍生物、聚乙烯醇類及其共聚物、丙烯酸 酉旨及甲基丙婦酸酉旨。 將凝膠施於或塗於皮膚上或導入體腔中。凝膠係藉由以 下方式來製備:用足量增稠劑處理如注射溶液之情形中所 述來製備之溶液,產生具有軟膏樣稠度之澄清材料。所採 用增稠劑係上文所給出之增稠劑。 將注施調配物傾注或噴灑在皮膚之所限定區域上,活性 133661.doc -138- 200917962 化合物渗透至皮膚中並以全身性方式作用。 注施調配物係藉由在適宜皮膚可相容溶劑或溶劑混合物 中溶解、懸浮或乳化活性化合物來製備。若適宜,可添加 其他辅助劑’例如著色劑、生物吸入促進物、抗氧化劑、 光穩定劑、黏著劑。 適宜溶劑係水、烷醇、二醇、聚乙二醇、聚丙二醇、甘 油、芳香族醇(例如笨甲醇、苯基乙醇、苯氧基乙醇)、酯 類(例如乙酸乙酯、乙酸丁酯、苯甲酸苄基酯)、醚類(例如 伸烷基二醇烷基醚,例如二丙二醇單甲基醚、二乙二醇單 丁基醚)、酮類(例如丙酮、甲基乙基酮)、環狀碳酸酯(例 如碳酸丙二酯、碳酸乙二酯)、芳香族及/或脂肪族烴、植 物油或合成油、DMF、二曱基乙醯胺、正烷基吡咯啶酮 (例如甲基対咬_、正了基料咬酮或正辛基吼洛咬 酮)、N-曱基吡咯啶酮、2_吡咯啶酮、2,2_二甲基_4_氧-亞 甲基-1,3-二氧戊環及甘油縮曱醛。 適宜著色劑係所有料用於動物且可料或料之著色 劑0 適宜吸收促進物係(例如)DMS〇、擴張油(例如肉豆蔻酸 異丙S曰)、一丙二醇壬酸酯、矽氧油及其與聚醚之共聚 物、脂肪酸酯、甘油三酯、脂肪醇。 適宜抗氧化劑係亞硫酸鹽或偏亞硫酸氫鹽⑼ϋ Μ 酸鉀)、抗壞血酸、丁經基甲苯、丁基經基菌香轉:、生; 酌·。 適宜光穩定劑係(例如)n〇vantis〇Hcacid。 133661.doc -139- 200917962 適宜黏著劑係(例如)纖維 稀酸醋、天然聚合物(例如萍酸乂物、殿粉衍生物、聚丙 眾馱鹽)、明膠。 f液可經口、經皮m射方式投與。 乳液係油包水型或水包油型。 其係藉由以下方式來製備· ^ ^ 將活性化合物溶於疏水或親 水相中’並在適宜乳化劑及Γ ^ &quot; 、且)其他辅助劑(例如著色 劑、吸收促進物質、防腐劑、 者色 增強物質)之辅助不將其盥1他黏度 ......他相之溶劑一起均質化。 適宜疏水相(油)係: ' 液體石蠛、石夕氧油、天然植物油(例如芝麻油、杏仁 油、說麻油)、合成甘油三_(例如辛酸/癸酸二甘油酿卜 與鏈長。8-。12之植物脂肪酸或其他特別選定天然脂肪酸之 甘油三S旨混合物、可能亦含有經基之飽和或不飽和脂肪酸 之偏甘油酯混合物、c8_Ci。脂肪酸之單甘油酯及二甘油 酿、脂肪酸酿(例如硬脂酸乙面旨、己二酸二正丁酸基醋、 月桂酸正己醇酯、二丙二醇壬酸酯)、中等鏈長之分支脂 肪酸與鏈長之飽和脂肪醇之酯類、肉豆蔻酸異丙 西曰彳示糊•異丙醋、鏈長Cu-C〗8之飽和脂肪醇的辛酸/癸 酸酯、硬脂酸異丙基酯、油酸油酯、油酸癸酯、油酸乙 醋、乳酸乙酯、蠟狀脂肪酸酯(例如合成鴨尾腺脂肪)、酞 酸二丁醋、己二酸二異丙基酯、及與後者相關之酯混合 物、脂肪醇(例如異十三烷醇、2-辛基十二烷醇、十六烷基 硬脂醯基醇、油醇)、及脂肪酸(例如油酸)及其混合物。 適宜親水相係:水、醇(例如丙二醇、甘油、山梨醇)及 133661.doc -140- 200917962 其混合物。 適宜乳化劑係: 非離子型表面活性劑,例如聚乙氧基化蓖麻油、聚乙氧 基化山木醇單油酸_、山梨醇單硬脂酸s旨、單硬脂酸甘油 s曰聚氧乙基硬脂酸酯、烷基酚聚乙二醇醚;兩性表面活 性劑,例如N-月士土盆说 月&amp;基-對亞胺基二丙酸二鈉或卵磷脂;陰 離子型表面活柯麻丨/£Ϊ .. 萬!例如十二烷基硫酸鈉、脂肪醇醚硫酸 酉旨、罕/ vJ^其 70 土 3k乙二醇醚正鱗酸酯單乙醇胺鹽;陽離子 活性表面活性劑,例如氣化十六烷基三曱基銨。 其他H«助劑係:可增強黏度並穩定乳液之物質,例 Μ曱基纖維素、曱基纖維素及其他纖維素及澱粉衍生 物聚丙烯自夂酉旨、藻酸鹽、明膠、阿拉伯樹膠、聚乙烤口比 口定7 士之亦台 Λ碲醇、甲基乙烯基醚與馬來酸酐之共聚物、 聚乙=醇、蠟、膠質矽酸或所提及物質之混合物。 广。于液可經口或局部’經皮投與。其係藉由以下方式來 ’ m生化合物懸浮於懸浮劑中,若適宜,其中添加 ”辅助j,例如潤濕劑、著色劑、生物吸收促進劑、防 腐劑、抗氧化劑、《穩定劑。 液體懸浮劑係所有均質溶劑與溶劑混合物。 適^閏濕劑(分散劑)係上文所給出之乳化劑。 可提及之其他輔助劑係上文所給出之彼等。 體製知丨可經口或局部’經皮投與。其與上述懸浮液 及乳液之不同之處僅在於其具有較高黏度。 對於固體製劑之生產,將活性化合物與適宜賦形劑思 133661.doc -141 - 200917962 口且右適宜添加輔助劑並製成期望形式。 用==劑係所有生理學上可财受的固體惰性物質。所 越(例二、“幾物及有機物。無機物係(例如)氣化納、碳酸 2 °奴酸鈣)、碳酸氫鹽、氧化鋁、氧化鈦 '矽酸、黏 撼::沈殿或膠質二氧切、或填酸鹽。有機物係(例如) 私、、維素、糧食及飼料(例如奶粉、動物粗粉、穀物粗 叙及碎屑、澱粉。 ^宜辅助劑係上文所提及之防腐劑、抗氧化劑、及/或 者色劑。 匕二他適且輔助劑係潤滑劑及助流劑(例如硬脂酸鎂、硬 脂酸、滑石粉、膨潤土)、促崩解物(例如殿粉或經交聯聚 烯比'⑷、黏合劑(例如殿粉、明膠或直鏈聚乙燦口比 各啶酮)、及幹式黏合劑(例如微晶纖維素卜 般而言,&quot;殺寄生蟲有效量”意指對生長達成可觀測效 應所需活性成份之量,料效應包括對壞死、死亡、滞 之放應、及去除、破壞或減小.1巴生物之出現率及 活性。對於本發明中所用各種化合物/組合物而言,殺寄 生触有效里可變。組合物之殺寄生蟲有效量亦可根據主要 條件(例如所期望殺寄生蟲效應及持續時間、靶物種、投 與模式及諸如此類)而變化。 本發明中所用組合物一般可包含約0.001-95°/〇的式1或π 化合物。 一般而言’有利地以0.5 mg/kg至100 mg/kg/天、較佳i mg/kgS50 mg/kg/天之總量施用式I或II化合物。 133661.doc -142- 200917962 之 曲p用ly中所合抵抗寄生蟲、較佳外寄生蟲之化合物、 =度為10沖⑺至如重量% ’較佳〇 重量%,更佳1_5〇重 量〇/° ’最佳5-40重量%。 、使用前經稀釋之製劑所含抵抗外寄生蟲之化合物之濃度 為〇_5’重量%,較佳1-50重量%。 此外製劑中所含抵抗内寄生蟲之式!或Η化合物之濃度 為 1〇 PPm_2 重罝%,較佳0.05-0.9 重量%,極佳〇·〇05_〇·25 重量%。 在本發明較佳實施例中包含式化合物之組合物係 經皮/局部施用。 在另-較佳實施例中’局部施用係以包含化合物之成型 物品形式來實&amp;,例如頸圈、圓飾物、耳標、固定於身體 局部之帶狀物、及黏著帶及箔片。 一般而言,有利地在三周療程内施用固體調配物,其以 10 mg/kg至 300 mg/kg、較佳2〇 mg/kgD〇〇 mg/kg、最佳 25 mg/kg至160 mg/kg經治療動物體重之總量來釋放式工或 II化合物。 對於成型物品之製備,使用熱塑性塑料及撓性塑料以及 彈性體及熱塑㈣性體。適宜塑料及彈性體係與式化 口物可充分相容的聚乙烯樹脂、聚胺基甲酸酯、聚丙烯酸 酿、環氧樹脂、、纖維素、纖維素衍生4勿、聚酿胺及聚酿。 用於成型物品之塑料及彈性體之詳表以及製備程序闡述於 (例如)WO 03/086075 中。 欲根據本發明使用之組合物亦可含有其他活性成份,例 133661.doc •143· 200917962 U权虫虫Μ、殺昆蟲劑、除草劑、殺真菌劑、或殺細菌 j肥料(例如硝酸録、展素 '卸驗、及過填酸鹽)、植物 毋素及植物生長調節劑、安全劑及殺線蟲劑。該等額外成 伤可依序使用或與上述組合物組合使用,若適宜亦可僅在 即將使用前添加(罐混合)。舉例而言,可在用其他活性成 份處理之河或之後用本發明組合物噴灑植物。 忒等忒劑可以1:10至1〇:1之重量比與本發明所用試劑混 合。將化合物I或Π或包含其之組合物以殺蟲劑使用形式與 其他殺蟲劑混合通常可達成更廣殺蟲作用範圍。 以下列表Μ展示可與本發明化合物丨或η 一起使用且使用 其可產生潛在協同效應之殺蟲劑,該列表意欲闡釋可能的 組合’但不施加任何限制: Μ.Ι.有機(硫代)磷酸鹽:高滅磷(acephate)、亞滅松 (azamethiphos)、益棉鱗(azinph〇s_ethyl)、保棉碟 (azinphos-methyl)、氯氧鱗(chlorethoxyfos)、氣芬碟 (chlorfenvinphos)、氣甲磷(chl〇rmephos)、毒死蜱 (chlorpyrifos)、甲基毒死蜱(chlorpyrifos-methyl)、庫馬磷 (coumaphos)、殺螟腈(cyanophos)、硫趕式甲基内吸碟 (demeton-S-methyl)、敵匹硫填(diazinon)、敵敵畏 (dichlorvos)/ DDVP 、百治填(dicrotophos)、樂果 (dimethoate)、曱基毒蟲畏(dimethylvinphos)、乙拌碟 (disulfoton) EPN 、乙硫填(ethion)、丙線碟 (ethoprophos)、胺續填(famphur)、苯線填(fenamiphos)、 殺模松(fenitrothion)、倍硫填(fenthion)、氟定菌碟 133661.doc -144- 200917962 (flupyrazophos)、嘆 °坐鱗(fosthiazate)、庚稀填 (heptenophos)、噁唑填(isoxathion)、馬拉硫填 (malathion)、滅财麟(mecarbam)、曱胺填 (methamidophos)、殺撲鱗(methidathion)、速滅填 (mevinphos)、久效構(monocrotophos)、三溴麟(naled)、氧 樂果(omethoate)、亞職構(oxydemeton-methyl)、對硫填 (parathion)、甲基對硫碟(parathion-methyl)、稻豐散 (phenthoate)、曱拌鱗(phorate)、伏殺碗(phosalone)、亞胺 硫鱗(phosmet)、填胺(phosphamidon)、肪硫磷(phoxim)、 甲基0密咬麟(pirimiphos-methyl)、丙溴磷(profenofos)、胺 丙畏(propetamphos)、丙硫填(prothiofos)、°比唾硫石粦 (pyraclofos)、必芬松(pyridaphenthion)、喧鳴琳 (quinalphos)、治棋麟(sulfotep) 、 丁基0^ 咬填 (tebupirimfos)、替美鱗(temephos)、特丁墻(terbufos)、司 替羅填(tetrachlorvinphos)、曱基乙拌破(thiometon)、三。坐 石粦(triazophos)、三氯石舞酸醋(trichlorfon)、财滅多 (vamidothion); Μ.2.胺基甲酸酯:涕滅威(aldicarb)、棉鈴威 (alanycarb) 、 °惡蟲威(bendiocarb)、丙硫克百威 (benfuracarb) 、 丁叉威(butocarboxim)、丁酿)颯威 (butoxycarboxim)、胺曱萘(carbaryl)、蟲瞒威 (carbofuran)、丁硫克百威(carbosulfan)、乙硫苯威 (ethiofencarb)、仲 丁威(fenobucarb)、伐蟲牌 (formetanate) 、 °夫線威(furathiocarb)、異丙威 133661.doc -145 - 200917962 (isoprocarb)、滅蟲威(methiocarb)、滅多蟲(methomyl)、速 滅威(metolcarb)、草胺醯(oxamyl)、抗財威(pirimicarb)、 曱基鄰異丙氧基氨基曱酸苯酯(propoxur)、硫雙威 (thiodicarb)、久效威(thiofanox)、混殺威(trimethacarb)、 XMC、滅殺威(xylylcarb)、。坐財威(triazamate); 1^.3.除蟲菊素類:氟丙菊酯(&amp;^11&amp;1;]11411)、丙烯除蟲菊 (allethrin)、右旋-順-反丙烯除蟲菊、右旋-反丙烯除蟲 菊、聯苯菊酯(bifenthrin)、反丙稀除蟲菊(bioallethrin)、 S-環戊稀基反丙烯除蟲菊、除蟲菊酯(bioresmethrin)、乙 氰菊酯(cycloprothrin)、氟氣氰菊酯(cyfluthrin)、冷·氟氯 氰菊酯、功夫菊酯(cyhalothrin)、λ-氟氣氰菊酯、7-氟氯 氰菊酯、氯氰菊酯(cypermethrin)、α-氣氰菊酯、卢-氯氰 菊酯、Θ-氣氰菊酯、ζ-氯氰菊酯、苯醚氰菊酯 (cyphenothrin)、漠氣菊醋(deltamethrin)、右旋稀炔菊醋 (empenthrin)、殺滅阿菊醋(esfenvalerate)、依芬普司 (etofenprox)、甲氰菊酯(fenpropathrin)、氰戊菊酯 (fenvalerate)、氟氰菊酯(flucythrinate)、氟氣笨菊酯 (flumethrin)、τ-氟胺氰菊酯(tau-fluvalinate)、苄蟎醚 (halfenprox)、依普寧(imiprothrin)、撲滅司林 (permethrin)、苯氧司林(phenothrin)、炔稀菊酯 (prallethrin)、苄0夫菊酯(resmethrin)、RU 1 5525、西拉福 芬(silafluofen)、七氟菊酉旨(tefluthrin)、四甲司林 (tetramethrin)、四溴菊酯(tralomethrin)、四氟笨菊酯 (transfluthrin)、ZXI 8901 ; 133661.doc -146- 200917962 M.4.擬保幼激素:稀蟲乙酯(hydroprene)、浠蟲炔酯 (kinoprene) 曱氧普烯(methoprene)、苯醚威 (fenoxycarb)、蚊繩&amp;| (pyriproxyfen); Μ. 5.煙驗性受體激動劑/抬抗劑化合物:咬蟲脉 (acetamiprid)、殺蟲磺(bensultap)、殺堵丹(cartap hydrochloride)、可尼丁 (clothianidin)、達特南 (dinotefuran) 、 11比蟲琳(imidacloprid)、賽速安 (thiamethoxam)、尼藤 D比藍(nitenpyram)、尼古丁 (nicotine)、賜諾殺(spinosad)(變構性激動劑)、《塞蟲琳 (thiacloprid)、殺蟲環(thiocyclam)、殺蟲單(thiosultap-sodium)及 AKD1022。 M.6. GABA門控氯離子通道拮抗劑化合物:氯丹 (chlordane)、硫丹(endosulfan)、7 -HCH(林丹(lindane)); 乙醢蟲腈(acetoprole)、伊希普(ethiprole)、氟蟲腈 (fipronil)、比氟普魯(pyrafluprole)、比普魯(pyriprole)、 凡尼力普魯(vaniliprole)、式Μ6· 1苯基》比。坐化合物For oral administration of warm-blooded animals, the compounds of formula I or II can be formulated into animal feed, animal feed premix, animal feed tumbling, pellets, solutions, ointments, suspensions. , veterinary use of drugs, gel, (four) Bu Da pills and capsules. Alternatively, the compound of formula I or π can be administered in the form of drinking water | animal. For oral administration of 'selected dosage forms, animals should be given 0.01 mg/kg to (10) called (10) animal weight/day of the formula or „compound, preferably from 05 mg/kg to 100 mg/kg animal body weight/day. The compound can be administered to the animal parenterally (for example by intratumor, intramuscular, intravenous or subcutaneous injection). The formula compound can be dispersed or dissolved in a physiologically acceptable carrier. For subcutaneous injection. Or 'the compound can be formulated as an implant for subcutaneous administration. In addition, the compound can be administered to the animal transdermally. For parenteral administration, the selected dosage form should be administered to the animal. A compound of formula 1 or II is provided in a concentration of 0.01 to 1 in cent. of the animal. The compound of formula I or II can also be applied topically to the animal in the form of a powder, a powder, a circle of love, a charm, Spraying agent, shampoo, spot application 133661 .doc -136· 200917962 and note S-wedding, and ointment or oil-in-water or water-in-oil emulsion. For topical application, infusions and sprays usually contain 0.5 ppm. Up to 5 〇〇〇ppm and preferably i ppm to 3 000 ppm In addition, formula compounds can be formulated into ear tags for animals (especially tetrapods such as cattle and sheep). Suitable formulations are: solutions, such as oral solutions, orally administered concentrates after dilution, for application to the skin or body cavity. Solution, formulation, gel; emulsion or suspension for oral or transdermal administration; semi-solid preparation; preparation of active compound by ointment-based or oil-in-water or water-in-oil emulsion base; solid Formulations, for example, powders, premixes or concentrates, granules, tablets, lozenges, boluses, capsules; aerosols and inhalants, and shaped articles containing active compounds. Suitable compositions for injection by active ingredients Prepare in a suitable solvent and add other ingredients such as acids, bases, buffer salts, preservatives, and solubilizers as needed. Sterile filtration and filling of the solution. Suitable solvents are physiologically tolerant solvents, such as Water, alkanols such as ethanol, butanol, stupid methanol, glycerol, propylene glycol, polyethylene glycol, hydrazine-methylpyrrolidone, 2-pyrrolidone, and mixtures thereof. The active compound may be dissolved in a physiologically tolerable vegetable oil or synthetic oil suitable for injection, as appropriate. Suitable and bulking agents are those which promote dissolution or prevent precipitation of the active compound in the main solvent. Vinyl pyrrolidone, "vinyl alcohol, polyoxyethylated castor oil, and polyoxyethylated sorbitan ester. 133661.doc -137- 200917962 Suitable preservatives are benzyl alcohol _ ιΤ τ and 虱Fermentation, parabens, and the butanol.: The solution is directly administered. After pre-dilution to the concentration used, oral administration, % of the solution, oral solution and concentrate are according to the current technology and the needle solution as above The method is prepared to make the sterilization process unnecessary. The solution used on the skin is sprayed, coated, rubbed, sprinkled or sprayed onto the skin. The solution for application to the skin is prepared according to the current techniques and as described above for the injection solution. The disinfection process is not required. Other suitable solvents are polypropylene glycol, phenylethyl alcohol, phenoxyethanol, esters (for example, acetic acid s or butyl acetate, benzoic acid f-based s), _ (for example, stretching / mono-alcohol alkyl ether) 'eg dipropylene glycol monomethyl ether), ketones (eg acetone, methyl ethyl ketone), aromatic hydrocarbons, vegetable oils and synthetic oils, dimethylformamide, dimethyletheneamine, ethylene glycol monoethyl _ 、, 嗣 嗣 glycerol (solkeul), propylene carbonate, and mixtures thereof. \ During the preparation period, it is better to add _ ^ suitable to increase (four) series: inorganic thickeners such as bentonite, colloidal tannic acid, aluminum monostearate; organic two additives, such as cellulose derivatives, polyvinyl alcohols and Its copolymer, acrylic acid and methyl acetoacetate are intended. The gel is applied to or applied to the skin or into the body cavity. The gel is prepared by treating a solution prepared as described in the case of an injection solution with a sufficient amount of a thickening agent to produce a clear material having an ointment-like consistency. The thickener used is the thickener given above. The formulation is poured or sprayed onto a defined area of the skin, activity 133661.doc -138- 200917962 The compound penetrates into the skin and acts in a systemic manner. The formulations are prepared by dissolving, suspending or emulsifying the active compound in a suitable skin compatible solvent or solvent mixture. If appropriate, other adjuvants such as coloring agents, biological inhalation enhancers, antioxidants, light stabilizers, and adhesives may be added. Suitable solvents are water, alkanol, diol, polyethylene glycol, polypropylene glycol, glycerin, aromatic alcohols (such as stupid methanol, phenylethanol, phenoxyethanol), esters (such as ethyl acetate, butyl acetate) , benzyl benzoate), ethers (such as alkylene glycol alkyl ethers, such as dipropylene glycol monomethyl ether, diethylene glycol monobutyl ether), ketones (such as acetone, methyl ethyl ketone) ), cyclic carbonates (eg, propylene carbonate, ethylene carbonate), aromatic and/or aliphatic hydrocarbons, vegetable oils or synthetic oils, DMF, dimethyl decylamine, n-alkyl pyrrolidone (eg Methyl sputum _, positive base ketone or n-octyl carbaryl ketone), N-decyl pyrrolidone, 2 pyrrolidone, 2,2 dimethyl _4 _ oxygen - methylene Base-1,3-dioxolane and glycerol formal. Suitable colorants are all materials used in animals and can be used as feedstocks. Suitable absorption systems are, for example, DMS(R), expansion oils (eg, isopropyl sulfonium myristate), propylene glycol phthalate, oxime Oil and its copolymer with polyether, fatty acid esters, triglycerides, fatty alcohols. Suitable antioxidants are sulfite or metabisulfite (9) potassium citrate), ascorbic acid, butyric acid toluene, butyl group-based bacteria:: raw; Suitable light stabilizers are, for example, n〇vantis〇Hcacid. 133661.doc -139- 200917962 Suitable adhesives are, for example, fiber sulphuric acid vinegar, natural polymers (such as barium sulphate, temple powder derivatives, polyacrylic acid salts), gelatin. The f solution can be administered by mouth or percutaneous injection. The emulsion is either a water-in-oil or an oil-in-water type. It is prepared by dissolving the active compound in a hydrophobic or hydrophilic phase, and in a suitable emulsifier and oxime, and other adjuvants (eg, coloring agents, absorption enhancing substances, preservatives, The aid of the color-enhancing substance does not 盥1 his viscosity...the solvent of the other phase is homogenized together. Suitable hydrophobic phase (oil) system: 'Liquid Dendrobium, Shishi Oxygen Oil, natural vegetable oil (such as sesame oil, almond oil, sesame oil), synthetic glycerol _ (such as caprylic acid / citric acid diglycerin brewing and chain length. 8 - 12 plant fatty acids or other specially selected natural fatty acid glycerol trisole mixtures, may also contain a mixture of saturated or unsaturated fatty acid glycerol esters, c8_Ci. fatty acid monoglycerides and diglycerols, fatty acids (eg stearic acid ethyl hexahydrate, di-n-butyric acid adipic acid vinegar, hexyl hexanoate, dipropylene glycol phthalate), medium chain length branched fatty acids and chain length saturated fatty alcohol esters, meat Isoprozil mesylate paste: isopropyl vinegar, chain length Cu-C〗 8 octanoic acid / phthalic acid ester of saturated fatty alcohol, isopropyl stearate, oleic acid ester, oleic acid oleate, Ethyl oleate, ethyl lactate, waxy fatty acid esters (eg synthetic duck tail fat), dibutyl citrate, diisopropyl adipate, ester mixtures associated with the latter, fatty alcohols (eg Isotridecyl alcohol, 2-octyldodecanol, cetyl Lipidyl alcohol, oleyl alcohol), and fatty acids (such as oleic acid) and mixtures thereof. Suitable hydrophilic phase: water, alcohol (such as propylene glycol, glycerin, sorbitol) and 133661.doc -140- 200917962 mixture thereof. Dosage system: non-ionic surfactants, such as polyethoxylated castor oil, polyethoxylated mountain aldol monooleic acid _, sorbitol monostearic acid s, monostearic acid glycerol s 曰 polyoxyethylene Alkyl stearate, alkylphenol polyglycol ether; amphoteric surfactant, such as N-moons earth basin, month & base-p-iminodipropionate disodium or lecithin; anionic surface activity柯麻丨/£Ϊ .. million! For example, sodium lauryl sulfate, fatty alcohol ether sulfate, / / vJ^70 soil 3k glycol ether orthophosphate monoethanolamine salt; cationic active surfactant For example, gasified cetyltrimethylammonium. Other H« adjuvants: substances that enhance viscosity and stabilize emulsions, such as fluorenyl cellulose, sulfhydryl cellulose and other cellulose and starch derivatives Since the purpose, alginate, gelatin, gum arabic, poly-baked mouth is more than 7 Also a copolymer of metocol, methyl vinyl ether and maleic anhydride, polyethylene=alcohol, wax, colloidal acid or a mixture of the substances mentioned. Widely. The liquid can be administered orally or locally. And the following is a method in which the compound is suspended in a suspending agent, and if appropriate, an auxiliary j is added, such as a wetting agent, a coloring agent, a bioabsorption promoter, a preservative, an antioxidant, and a stabilizer. The liquid suspension is a mixture of all homogeneous solvents and solvents. Suitable moisturizers (dispersants) are the emulsifiers given above. Other adjuvants which may be mentioned are those given above.丨 can be administered orally or locally 'transdermally. It differs from the above suspensions and emulsions only in that it has a higher viscosity. For the production of solid preparations, the active compound and suitable excipients are considered 133661.doc - 141 - 200917962 The right and appropriate adjuvants are added to the mouth and made into the desired form. Use the == agent for all physiologically acceptable solid inert substances. The more (Example 2, "Several substances and organic matter. Inorganic systems (for example) gasification sodium, 2 ° calcium carbonate citrate), bicarbonate, alumina, titanium oxide 'tannic acid, sticky:: Shen Dian or colloid II Oxygen-cut, or acid-filled. Organic systems (for example) private, vitamins, grain and feed (eg milk powder, animal meal, coarse grain and crumbs, starch.) Adjuvants are mentioned above Preservatives, antioxidants, and/or colorants. Hydrogen and adjuvants (such as magnesium stearate, stearic acid, talc, bentonite), disintegration (such as temples) Powder or cross-linked polyene ratio '(4), adhesive (such as temple powder, gelatin or linear polyacetate than hexanone), and dry binder (such as microcrystalline cellulose), &quot; An effective amount of parasiticidal means the amount of active ingredient required to achieve an observable effect on growth, including effects on necrosis, death, stagnation, and removal, destruction or reduction. For the various compounds/compositions used in the present invention, the parasitic touch is effective. The parasiticidally effective amount of the composition may also vary depending on the primary conditions (e.g., desired parasiticidal effect and duration, target species, mode of administration, and the like). The compositions used in the present invention may generally comprise from about 0.001 to about 95. Compound of formula 1 or π of °/〇. In general, the compound of formula I or II is advantageously applied in a total amount of from 0.5 mg/kg to 100 mg/kg/day, preferably i mg/kg S50 mg/kg/day. 133661.doc -142- 200917962 The song p is compounded with ly resistant parasites, preferably ectoparasites, with a degree of 10 rush (7) to a weight % 'better 〇 weight %, more preferably 1 _ 5 〇 weight 〇 /° 'Optimum 5-40% by weight. The concentration of the compound resistant to ectoparasites contained in the diluted preparation before use is 〇_5'% by weight, preferably 1-50% by weight. Further resistance contained in the preparation The concentration of the endoparasite! or the hydrazine compound is 1 〇PPm 2 罝%, preferably 0.05-0.9% by weight, excellent 〇·〇05_〇·25% by weight. In the preferred embodiment of the invention, the inclusion formula The composition of the compound is administered transdermally/topically. In another preferred embodiment, the topical application is in the form of a package. The form of the shaped article containing the compound is applied to, for example, a collar, a round ornament, an ear tag, a band attached to the body part, and an adhesive tape and a foil. In general, it is advantageous to apply solids within a three-week course of treatment. Formulation, which is released at a total weight of 10 mg/kg to 300 mg/kg, preferably 2 mg/kg D〇〇mg/kg, and optimally 25 mg/kg to 160 mg/kg of treated animal body weight Or II compound. For the preparation of shaped articles, thermoplastics and flexible plastics, as well as elastomers and thermoplastics (tetra), suitable for plastics and elastomers, and polyethylene resins and polyamines, which are fully compatible with the formula. Acid ester, polyacrylic acid brewing, epoxy resin, cellulose, cellulose derivative 4, poly-bristamine and poly-brew. A detailed list of plastics and elastomers for forming articles and preparation procedures are set forth, for example, in WO 03/086075. Compositions intended for use in accordance with the present invention may also contain other active ingredients, for example, 133661.doc • 143·200917962 U worms, insecticides, herbicides, fungicides, or bactericidal fertilizers (eg, nitrates, Exhibitors 'unloading, and over-filling salts), phytochemicals and plant growth regulators, safeners and nematicides. These additional wounds may be used sequentially or in combination with the above compositions, and may be added just prior to use (tank mixing) if appropriate. For example, the plants can be sprayed with the compositions of the invention after or after treatment with other active ingredients. The tanning agent can be mixed with the reagent used in the present invention in a weight ratio of 1:10 to 1 :1. Mixing Compound I or hydrazine or a composition comprising the same with other insecticides in the form of insecticide use generally achieves a broader range of insecticidal action. The following list Μ shows insecticides that can be used with the compounds 丨 or η of the present invention and which can be used to produce potential synergistic effects. The list is intended to illustrate possible combinations 'without any restrictions: Μ.Ι.Organic (thio) Phosphate: acephate, azamethiphos, azinph〇s_ethyl, azinphos-methyl, chlorethoxyfos, chlorfenvinphos, gas Chymium (Chl〇rmephos), chlorpyrifos, chlorpyrifos-methyl, coumaphos, cyanophos, demeton-S-methyl ), diazinon, dichlorvos / DDVP, dicrotophos, dimethoate, dimethylvinphos, disulfoton EPN, ethyl sulphur (ethion), exthoprophos, famphur, fenamiphos, fenitrothion, fenthion, fluorosis 133661.doc -144- 200917962 (flupythiaophos), sigh ° sitting scales (fosthiazate) Heptenophos, isoxathion, malathion, mecarbam, methamidophos, methidathion, mevinphos, Monocrotophos, naled, omethoate, oxydemeton-methyl, parathion, parathion-methyl, rice Phenthoate, phorate, phosalone, phosmet, phosphamidon, phoxim, pirimiphos-methyl ), profenofos, propetamphos, prothiofos, pyrracofos, pyridaphenthion, quinalphos, zhiqilin Sulfotep), butyl 0^ bite (tebupirimfos), temephos, terbufos, tetrachlorvinphos, thiometon, three. Sitting on triazophos, trichlorfon, vamidothion; Μ.2. urethane: aldicarb, alanycarb, ° (bendiocarb), benfuracarb, butocarboxim, butadiene, butoxycarboxim, carbaryl, carbofuran, carbosulfan ), ethiofencarb, fenobucarb, formetanate, furathiocarb, isoprocarb 133661.doc -145 - 200917962 (isoprocarb), chlorpyrifos ( Methiocarb), methomyl, metolcarb, oxamyl, pirimicarb, propoxur, thiodicarb ( Thiodicarb), thiofanox, trimethacarb, XMC, xylylcarb. Take triazamate; 1^.3. Pyrethrins: flumethrin (&amp;^11&amp;1;]11411), pyrethroid (allethrin), dextro-cis-trans propylene Cordyceps, dextro-pyridyl pyrethrum, bifenthrin, bioallethrin, S-cyclopentyl anti-propylene pyrethrum, pyrethrin (bioresmethrin), Cycloprothrin, cyfluthrin, cold cyfluthrin, cyhalothrin, lambda-cyfluthrin, 7-cyfluthrin, cypermethrin, alpha-gas Cypermethrin, cypermethrin, Θ-cypermethrin, ζ-cypermethrin, cyphenothrin, deltamethrin, empenthrin, killing Aju Esfenvalerate, etofenprox, fenpropathrin, fenvalerate, flucythrinate, flumethrin, τ-fluoroamine Tau-fluvalinate, halfenprox, imiprothrin, permethrin, phenoxyline (p Henothrin), prallethrin, resmethrin, RU 1 5525, silafluofen, tefluthrin, tetramethrin, tetra Tralomethrin, transfluthrin, ZXI 8901; 133661.doc -146- 200917962 M.4. Probiotic hormones: hydroprene, kinoprene Methoprene, fenoxycarb, mosquito rope &amp;| (pyriproxyfen); Μ. 5. Smoking receptor agonist/antibodal compound: acetamiprid, insecticidal Bensultap, cartap hydrochloride, clothianidin, dinotefuran, 11 imidacloprid, thiamethoxam, nitenpy blue (nitenpyram) , nicotine, spinosad (allosteric agonist), thiacloprid, thiocyclam, thiosultap-sodium, and AKD 1022. M.6. GABA-gated chloride channel antagonist compounds: chlordane, endosulfan, 7-HCH (lindane); acetoprole, ethiprole , fipronil (fipronil), than pyraproll (pyrafluprole), pyriprole, vaniliprole (vaniliprole), formula Μ 1-6 phenyl. Sitting compound

Ο SΟ S

Μ.7.氣離子通道活化劑:阿巴克丁(abamectin)、埃瑪 菌素(emamectin benzoate)、密滅汀(milbemectin)、萊培菌 素(lepimectin); 133661.doc -147- 200917962 Μ·8. ΜΕΤΙ I化合物:啥蜗醚(fenazaquin)、。坐蜗S旨 (fenpyroximate) 11 密蜗 (pyrimidifen)、健蜗靈 (pyridaben) 、 D比蜗胺(tebufenpyrad) 、 °坐蟲醯胺 (tolfenpyrad)、氟酚瑞姆(fiufenerim)、魚藤酮(r〇ten〇ne); M.9. METI II及 III化合物:阿色奎西(aceqUjn〇Cyi)、普 克赛姆(fluacyprim)、氟蟻腙(hydrarnethylnon); Μ· 1 0.氧化填酸化之解偶聯劑:蟲蜗猜(chi〇rfenapyr)、 DNOC ; Μ. 11 ·氧化鱗酸化之抑制劑:三。坐錫(az〇CyCi〇tin)、三 環錫(cyhexatin)、丁喊脲(diafenthiuron)、苯丁錫 (fenbutatin oxide)、快蜗特(pr〇pargjte)、四氣殺蜗石風 (tetradifon); M.12.蜆皮干擾劑.環丙馬秦(Cyr〇mazine)、可芬諾 (chromafenozide)、_ 芬載(hai〇fenozide) ' 甲氧芬载 (methoxyfenozide)、得布芬載(tebufenozide); M.13.協同劑.胡椒基丁趟(piper〇nyi butoxide) '脫葉 填(tribufos); M.I4·鈉通道阻斷劑化合物:引多沙克(ind〇xacarb)、 美氟膝(metaflumizone); M.15.熏蒸劑:曱基溴、氣化苦磺醯氟(chl〇r〇picrin sulfuryl fluoride); Μ·16.選擇性飼喂阻斷劑:冰晶石(cryi〇tie)、拒嗓酮 (pymetrozine)、氟啶蟲醯胺(fl〇nicamid); Μ· 1 7.蜗蟲生長抑制劑:四蜗喚(ci〇fentezine)、β塞蜗酮 133661.doc -148· 200917962 (hexythiazox)、伊妥。惡嗤(etoxazole); Μ· 1 8.殼多糖合成抑制劑.:η塞嘻酮(buprofezin)、雙三氣 蟲脲(bistrifluron)、氟啶脲(chlorfluazuron)、二氟苯隆 (diflubenzuron)、氟環脲(flucycloxuron)、氟蟲腺 (flufenoxuron)、氟鈴脲(hexaflumuron)、氯芬奴隆 (lufenuron)、諾華隆(novaluron)、多氟1脲(11〇¥1!'111]11111·。]!)、 氟苯脲(teflubenzuron)、殺鈴腺(triflumuron); Μ.19. 脂質生物合成抑制劑:螺二克芬 (spirodiclofen)、螺曱蜗 g旨(spiromesifen)、螺蟲乙醋 (spirotetramat); Μ.20. 八胺能(Octapaminergic)激動劑:三亞蝴 (amitraz) ί Μ·21.蘭尼驗(Ryanodine)受體調節劑:氟蟲酿胺 (flubendiamide); M.22.多種:填化鋁、醯胺氟米特(amidoflumet)、苯克 魯賽兹(benclothiaz)、苯蜗特(benzoximate)、畢芬載 (bifenazate)、硼砂(borax)、漠瞒醋(bromopropylate)、乳 化物、賽諾若紛(cyenopyrafen) 、 丁 H蜗西旨 (cyflumetofen)、滅滿猛(chinomethionate)、開樂散 (dicofol)、氟乙酸酯、磷化氫、啶蟲丙醚(pyridalyl)、比氟 嗤腙(pyrifluquinazon)、硫、有機硫化合物、吐酒石(tartar emetic)、績醯亞胺化合物Μ22· 1, 133661.doc -149- 200917962Μ.7. Air ion channel activator: abamectin, emamectin benzoate, milbemectin, lepimectin; 133661.doc -147- 200917962 Μ· 8. ΜΕΤΙ I compound: fenazaquin.芬pyroximate 11 pyrimidifen, pyridaben, D than tebufenpyrad, tolfenpyrad, fiufenerim, rotenone (r〇 Ten〇ne); M.9. METI II and III compounds: aceqUjn〇Cyi, fluacyprim, hydrarnethylnon; Μ·1 0. Oxidation and acidification solution Coupling agent: chi〇rfenapyr, DNOC; Μ. 11 · Inhibitor of oxidative sulphation: three. Sitting on tin (az〇CyCi〇tin), cyhexatin, diafenthiuron, fenbutatin oxide, pr〇pargjte, tetradifon M.12. Quercemic interfering agent. Cyr〇mazine, chromafenozide, _ 芬 〇 oz oz ' ' methoxy methoxy methoxy methoxy methoxy methoxy methoxy methoxy methoxy methoxy methoxy methoxy methoxy methoxy te te te te te te te te te te M.13. Synergistic agent. Piper〇nyi butoxide 'tribufos'; M.I4·sodium channel blocker compound: Indoxacarb, US fluoride Metaflumizone; M.15. fumigant: mercapto bromide, chl〇r〇picrin sulfuryl fluoride; Μ·16. selective feeding blocker: cryolite (cryi〇tie ), pymetrozine, fl〇nicamid; Μ·1 7. Insulin growth inhibitor: ci〇fentezine, β serotonin 133661.doc -148· 200917962 (hexythiazox), Ito. Etoxazole; Μ·1 8. Chitin synthesis inhibitors: probuprofen (buprofezin), bistrifluron, chlorfluazuron, diflubenzuron, Flucycloxuron, flufenoxuron, hexaflumuron, lufenuron, novaluron, polyfluoro 1 urea (11〇¥1!'111]11111· .]!), flubenzuron (teflubenzuron), triflumuron; Μ.19. Lipid biosynthesis inhibitors: spirodiclofen, spiromesifen, snail vinegar (spirotetramat); Μ.20. Octapaminergic agonist: amitraz ί Μ 21. Ryanodine receptor modulator: flubendiamide; M.22. A variety of: filled aluminum, amidoflumet, benclothiaz, benzoximate, bifenazate, borax, bromopropylate, Emulsion, cyenopyrafen, cyflumetofen, chinomethionate, Difolf, fluoroacetate, phosphine, pyridalyl, pyrifluquinazon, sulfur, organic sulfur compounds, tartar emetic, bismuth imine compounds Μ22· 1, 133661.doc -149- 200917962

N-CN cr n (M22.1) M22.2, crN-CN cr n (M22.1) M22.2, cr

O N-CN (M22·2)O N-CN (M22·2)

或 M22.3, 嘧啶基炔基醚化合物M22.4或噻二唑基炔基醚化合物 M22.5,Or M22.3, pyrimidinyl alkynyl ether compound M22.4 or thiadiazolyl alkynyl ether compound M22.5,

M22·5 其中RM-22係甲基或乙基且Het*係3,3-二曱基吡咯啶-1-基、3-甲基六氫吡啶-1-基、3,5-二甲基六氫吡啶-1-基、3-三氟曱基六氫吡啶-1-基、六氫氮呼-1-基、2,6-二曱基六氫 氮呼-1-基或2,6-二曱基嗎琳-4 -基; M,23. N-R;-2,2-二鹵代-1-R&quot;環-丙烷曱醯胺_2_(2,6_二氯· α,α,α-三氟-對甲苯基)腙或N-R,-2,2-二(R'M)丙醯胺-2-(2,6-二 氣-α,α,α-三 氟-對 曱苯基)-腙 ,其中 R,係甲 基 或乙基 ,鹵 素係氯或溴,R’’係氫或甲基且R&quot;·係甲基或乙基; M.24.胺基苯醯胺·· Chloranthraniliprole、式 M24.1 化 合物 133661.doc -150- 200917962M22·5 wherein RM-22 is methyl or ethyl and Het* is 3,3-dimercaptopyrrolidin-1-yl, 3-methylhexahydropyridin-1-yl, 3,5-dimethyl Hexahydropyridin-1-yl, 3-trifluorodecylhexahydropyridin-1-yl, hexahydroazin-1-yl, 2,6-dimercaptohexahydroazin-1-yl or 2,6 - 曱 吗 吗 -4 -4 - 4 - base; M, 23. NR; -2,2-dihalo-1-R&quot; cyclopropane oxime 2_(2,6-dichloro-α,α, Α-trifluoro-p-tolyl) oxime or NR,-2,2-di(R'M)propanamide-2-(2,6-di-gas-α,α,α-trifluoro-p-nonylbenzene Base)-腙, wherein R is methyl or ethyl, halogen is chlorine or bromine, R'' is hydrogen or methyl and R&quot; is methyl or ethyl; M.24. Aminophenylamine · Chloranthraniliprole, formula M24.1 compound 133661.doc -150- 200917962

Μ.25.丙二腈化合物:CF2HCF2CF2CF2CH2C(CN)2 CH2CH2CF3、(2-(2,2,3,3,4,4,5,5-八氟戊基)-2-(3,3,3-三氟-丙基)丙二腈)、〇?3((:1^2)2(:(€]^)2(:112(〇卩2)50?2^1、(2-(2,2,3,3,4,4,5,5,6,6,7,7 -十二乱庚基)-2-(3,3,3-三氣-丙基)_ 丙二腈)、CF3(CH2)2C(CN)2(CH2)2C(CF3)2F (2-(3,4,4,4-四 氟-3-三氟甲基-丁基)-2-(3,3,3-三氟-丙基)-丙二腈)、 CF3(CH2)2C(CN)2(CH2)2(CF2)3CF3 (2-(3,3,4,4,5,5,6,6,6_ 九 氟己基)-2-(3,3,3-三氟i -丙基)-丙二腈)、cf2H (CF2)3CH2C(CN)2CH2(CF2)3CF2H(2,2-雙-(2,2,3,3,4,4,5,5-八 氟戊基)-丙二腈)、CF3(CH2)2C(CN)2CH2(CF2)3CF3 (2_ (2,2,3,3,4,4,5,5,5-九氟戊基)-2-(3,3,3-三氟-丙基)_ 丙二 腈)、CF3(CF2)2CH2C(CN)2CH2(CF2)3CF2H (2-(2,2,3,3,4,4,4- 七氟-丁基)-2-(2,2,3,3,4,4,5,5-八氟戊基)-丙二腈)、 CF3CF2CH2C(CN)2CH2(CF2)3CF2H (2-(2,2,3,3,4,4,5,5-八氣 戊基)-2-(2,2,3,3,3-五氟-丙基)-丙二腈)、 CF2HCF2CF2CF2CH2C(CN)2CH2CH2CF2CF3(2-(2,2,3,3,4,4,5,5- 八氟戊基)-2-(3,3,4,4,4-五氟丁基)-丙二腈)、 CF3(CH2)2C(CN)2CH2(CF2)3CF2H (2-(2,2,3,3,4,4,5,5-八氟戊 基)-2-(3,3,3-三氟-丁基)-丙二猜); M.26.微生物干擾劑:蘇雲金芽孢桿菌以色列亞種 133661.doc -151 - 200917962 (Israelensi)、球形桿菌(Baciiius sphaericus)、蘇雲金芽孢 桿菌钻澤亞種(Aizawai)、蘇雲金芽孢桿菌庫斯克亞種 (Kurstaki)、I禾雲金芽孢桿菌擬步行曱亞種(Tenebri〇nis); 除其他出版物外’群組Μ之市售化合物可參見pesticideΜ.25. Malononitrile compound: CF2HCF2CF2CF2CH2C(CN)2 CH2CH2CF3, (2-(2,2,3,3,4,4,5,5-octafluoropentyl)-2-(3,3,3 -Trifluoro-propyl)malononitrile), 〇?3((:1^2)2(:(€]^)2(:112(〇卩2)50?2^1,(2-(2 , 2,3,3,4,4,5,5,6,6,7,7 -12-glyptyl)-2-(3,3,3-tris-propyl)-malononitrile , CF3(CH2)2C(CN)2(CH2)2C(CF3)2F (2-(3,4,4,4-tetrafluoro-3-trifluoromethyl-butyl)-2-(3,3 , 3-trifluoro-propyl)-malonitrile, CF3(CH2)2C(CN)2(CH2)2(CF2)3CF3 (2-(3,3,4,4,5,5,6, 6,6_ nonafluorohexyl)-2-(3,3,3-trifluoroi-propyl)-malononitrile), cf2H (CF2)3CH2C(CN)2CH2(CF2)3CF2H (2,2-bis- (2,2,3,3,4,4,5,5-octafluoropentyl)-malononitrile), CF3(CH2)2C(CN)2CH2(CF2)3CF3 (2_ (2,2,3, 3,4,4,5,5,5-nonafluoropentyl)-2-(3,3,3-trifluoro-propyl)-malononitrile, CF3(CF2)2CH2C(CN)2CH2(CF2 ) 3CF2H (2-(2,2,3,3,4,4,4-heptafluoro-butyl)-2-(2,2,3,3,4,4,5,5-octafluoropentyl) )-Malonitrile (CF2CF2CH2C) ,3,3-pentafluoro-propyl)-malononitrile), CF2HCF2CF2CF2CH2C(CN)2CH2CH2CF2CF3(2-(2,2,3,3,4,4,5,5 - octafluoropentyl)-2-(3,3,4,4,4-pentafluorobutyl)-malononitrile), CF3(CH2)2C(CN)2CH2(CF2)3CF2H (2-(2, 2,3,3,4,4,5,5-octafluoropentyl)-2-(3,3,3-trifluoro-butyl)-propanoid); M.26. Microbial Interfering Agent: Su Yunjin Bacillus Israel subspecies 133661.doc -151 - 200917962 (Israelensi), Baciiius sphaericus, Bacillus thuringiensis subspecies (Aizawai), Bacillus thuringiensis, Kurstaki, I. Breeding subspecies (Tenebri〇nis); among other publications, 'commercial compounds of the group can be found in pesticide

Manual ’ 弟 13 版 ’ British Crop Protection Council (2003) ° 式M6.1硫代醯胺及其製劑闡述於w〇 98/28279中。萊培 菌素揭示於 Agro pr0ject,pjB Publications有限公司,2〇〇4 年11月中。苯克魯赛茲及其製劑闡述於歐洲專利第EP-A1 45462 1中。殺撲璃及對氧鱗(para〇x〇n)及其製劑闡述於 Farm Chemicals Handbook,第 88卷,Meister Publishing公 司’ 2〇01中。乙醯蟲腈及其製劑闡述於WO 98/28277中。 美氟腙及其製劑闡述於歐洲專利第EP-A1 462 456號中。 0比氣硫構(Flupyrazofos)闡述於 Pesticide Science 54, 1988,第237-243頁及美國專利第4822779號中。比氟普魯 及其製劑闡述於曰本專利第2002193709號及WO 01/00614 中。比普魯及其製劑闡述於WO 98/45274及美國專利第 63 35357號中。醯胺氟米特及其製劑闡述於美國專利第 6221890號及日本專利第21010907號中。氟酚瑞姆及其製 劑闡述於 WO 03/007717 及 WO 03/007718 中。AKD 1022 及 其製劑闡述於美國專利第6300348號中。 Chloranthraniliprole 闡述於 WO 01/70671、WO 03/0155 19 及WO 05/11δ552中。式M24.1胺基苯醯胺衍生物闡述於 WO 01/70671、WO 04/067528 及 WO 05/1 18552 中。丁氟蟎 133661.doc -152- 200917962 酯及其製劑闡述於WO 04/080 180中。胺基喹唑啉酮化合物 比氟喹腙闡述於歐洲專利第A 109 7932號中。式M22 l、 M22.2或M22.3續醯亞胺衍生物或其類似物及其製備方法閣 述於WO 2006/060029中。炔基醚化合物M22.4及M22.5閣 述於(例如)日本專利第2006131529號中。有機硫化合物閣 述於WO 2007060839中。丙二腈化合物闡述於 02/089579、WO 02/090320、WO 02/090321 、 04/006677、WO 05/068423、WO 05/068432 及 W〇 05/063694 t ° 殺真菌混合配合物係選自由以下組成之群之彼等:酸基 丙胺酸’例如苯霜靈(benalaXyi)、甲霜靈(metalaxyi)、甲 吱酿胺(ofurace)、惡霜靈(oxadixyl);胺衍生物,例如阿迪 嗎啉(aldimorph)、多寧(dodine)、十二環嗎啉 (dodemorph)、丁 苯嗎琳(fenpr〇pim〇rph)、苯鏽 口定 (fenpropidin)、雙胍辛胺(guazatine)、培福朗 (iminoctadine)、螺噁胺(spir〇xamin)、十三嗎啉 (tridemorph),本%喷D定,例如二曱变 菌胺(pyrimethanil)、哺菌胺(mepanipyrim)或 eyr〇dinyi ;抗 生素,例如放線菌酮(cycl〇heximid)、灰黃黴素 (griseofulvin)、春雷黴素(kasugamyCin)、那他黴素 (natamycin) 夕抗黴素(polyox in)或鏈黴素 (streptomycin);唑類,例如聯苯三唑醇(bitertan〇i)、溴康 坐(bromoconazole)、環丙 0坐醇(Cypr〇c〇naz〇ie)、苯喊甲環 唑(difenoconazole)、烯唑醇(dinic〇na z〇le)、環氧康唑 133661.doc -153- 200917962 (epoxiconazole)、分菌氰唑(fenbuc〇nazole)、氟奎康唆 (fluquiconazole)、護矽得(flusilaz〇le)、己唑醇 (hexaconazole)、烯菌靈(imazalil)、葉菌嗅 (metconazole)、腈菌唑(myclobutanil)、配那。坐 (penconazole)、丙環。坐(propiconazole)、丙氣 * (prochloraz)、撲硫康。坐(pr〇thioconazole)、戊。坐醇 (tebuconazole)、三唑酮(triadimefon)、三唑醇 (triadimenol)、三氟咪唑(triflumizol)、滅菌唑 (triticonazole)、粉唑醇(flutriaf〇i);二羧甲醯亞胺,例如 異 il 脲(iprodion)、甲菌利(myclozolin)、腐黴利 (procymidon)、伐菌唑靈(vinci〇z〇iin);二硫代胺基甲酸 S旨,例如福美鐵(ferbam)、代森納(nabam)、代森鏟 (maneb)、代森猛鋅(mancozeb)、美坦(metam)、代森聯 (metiram)、丙森鋅 (propineb)、 代森福鎂鋅 (polycarbamate)、塞侖(thiram)、福鎂鋅(ziram)、乙硫鋅 (zineb) ’雜環化合物’例如敵菌靈(aniiazine)、苯菌靈 (benomyl)、波斯卡利(b〇scalid)、多菌靈(carbendazim)、 萎鏽靈(carboxin)、氧化萎鏽靈、嗟嗤滅(Cyazofamid)、福 美曱醋(dazomet)、 腈硫酿(dithianon)、 泛惡同 (famoxadon)、芬納米同(fenamid〇n)、樂必耕(fenarimol)、 麥穗寺(fuberidazole)、紋枯胺(flutolanil)、福拉比 (furametpyr)、稻盘靈(isoprothiolane)、滅鑛胺 (mepronil)、氟苯鳴0定醇(nuarimol)、稀丙苯°塞。坐 (probenazole)、普奎那茲(pr〇qUinazid)、消斑两 133661.doc -154- 200917962 (pyrifenox)、咯喹酮(pyroquilon)、奎諾克西芬 (quinoxyfen)、矽托凡(silthiofam)、噻苯健唾 (thiabendazole)、西福割麥(thifluzamid)、硫芬 g旨甲美 (thioph an at e-methyl)、替 丁 尼(tiadinil)、三環。坐 (tricyclazole)、嗪胺靈(triforine);銅殺真菌劑,例如波爾 多(Bordeaux)混合物、乙酸銅、氧氣化銅、鹼式硫酸銅; 瑞基苯基衍生物,例如樂殺蜗(binapacryl)、消蜗普 (dinocap)、敵蜗通(dinobuton)、硝基献基異丙基;苯基0比 口各’例如拌種略(fenpiclonil)或p各菌腈(fludioxonil);硫; 其他殺真菌劑,例如S-甲基阿西本唾(acibenzolar-S_ methyl)、本賽夫利卡(benthiavalicarb)、卡波帕麥 (carpropamid)、四氣異苯腈(chl〇rothalonil)、赛扶芬納米 (cyflufenamid)、霜脲氰(cymoxanil)、璉菌 _ (diclomezin)、大克賽美(diclocymet)、乙徽威 (diethofencarb)、敵瘟磷(edifen-phos)、衣沙布山 (ethaboxam)、環醯菌胺(fenhexamid)、乙酸三苯錫(fentin-acetate)、务 °惡尼(fenoxanil)、嘴菌腙(ferimzone)、氟 °定胺 (fluazinam)、福賽得(fosetyl)、福賽得鋁、衣普法利卡 (iprovalicarb)、六氣笨、美查芬隆(metrafen〇n)、賓克隆 (pencycuron)、普潘莫卡(pr〇parnocarb)、四氣苯献 (phthalide)、曱基特科拉夫斯(t〇i〇ci〇f〇s_methyl)、五氯硝 本(quintozene) 、 β坐沙麥(zoxamid);史卓比尿 (strobilurin),例如腈嘧菌g旨(az〇xystr〇bin)、二莫西史卓賓 (dimoxystrobin)、氟噁史卓賓(flu〇xastr〇bin)、苯氧菊酯 133661.doc -155- 200917962 (kresoxim-methyl)、苯氧菌胺(me_torninostrobin)、歐沙史 卓賓(orysastrobin)、比可西史卓賓(pic〇xystr〇bin)或肟菌 酯(trifloxystrobin);次磺酸衍生物,例如敵菌丹 (captafol)、蓋普丹(captan)、苯氟磺胺(dichlofluanid)、滅 菌丹(folpet)、對曱抑菌靈(t〇lylfluanid);肉桂醯胺及類似 物’例如烯醯嗎啉(dimethomorph)、It滅歐(flumetover)或 氟嗎琳(flumorph)。 可藉由業内已知的任何施用方法使無脊椎害蟲(即節肢 動物及線蟲)、植物、其中生長植物之土壤或水與本發明 化合物I或II或含有其之組合物接觸。由此,&quot;接觸&quot;包括直 接接觸(將化合物/組合物直接施用至無脊椎害蟲或植物上_ 通常施用至植物葉片、莖或根上)及間接接觸(將化合物/組 合物施用至無脊椎害蟲或植物之所在地)。 此外,可藉由使殺蟲有效量之式丨或^化合物與無害蟲、 其食物供應、棲息地、繁殖地或其所在地接觸來控制無脊 椎害蟲。由此,可在所在地、生長中之作物或已收穫作物 被害蟲感染之前或之後實施施用。 &quot;所在地’’意指害蟲或寄生蟲生長或可生長之棲息地、繁 殖地、栽培植物、植物繁殖材料(例如種子)、土壤、區 域、材料或環境。 一般而言,,,殺蟲有效量&quot;意指達成對生長之可觀測效應 (包括壞死、死亡、滯後、預防、及去除、破壞或減小靶 生物體之出現率及活性之效應)所需之活性成份量。對於 本發明中所用各種化合物/組合物而言,殺蟲有效旦 里 133661.doc •156· 200917962 變。組合物之殺蟲有效量亦 殺蟲效果及持續時間、天氣 及諸如此類)而改變。 了根據主要條件(例如所期望 、靶物種、所在地、施用模式 樹)合:及其組合物可用於保護木質材料(例如 :亦可用於保護建築材料、家具、皮革、纖維製品乙)稀 製品、電線及電境等免受轉蟻及/或白蟻侵害 =犧及白犧以使其不會對作物或人類造成傷害(例 田。蟲入铋房屋及公共設施時)。式工或Η化合物不僅 可施用至周圍土壤表面或地板下土壤,以保護木質材料, 且亦可將其施用至塊狀物品(例如地板下混凝土、壁櫥 柱、樑、膠合板、家具等之表面)、木質物品(例如:花 板半板等)及乙締製品(例如漆包電線、乙稀板、隔轨材 料(例如苯乙輸體)等)。在防紫螞蟻危害農作物或人類 之應用If况下’可將本發明之螞蟻控制劑施用至農作物上 或周圍土壤中’或直接施S至螞蟻巢穴中或諸如此類。 亦可預防性地將式w π化合物施用至預期害蟲會出現之 位置。 或II化合物亦可用於保護生長中之植物免受害蟲侵襲 或侵擾’其係藉由使該植物與殺蟲有效量之式wn化合物 接觸來實施。因此,,,接觸”包括直接接觸(將化合物/組合 物直接施用至害蟲及/或植物上_通常施用至植物葉片、莖 或根部)及間接接觸⑻匕合物/組合物施用i害蟲及/或^ 物所在地)。 133661.doc -157- 200917962 在土壤處理或施用至害蟲聚居地或巢穴之情況下,活性 成份之量介於0._!· g/1G() m2(較佳在請i2() g/i〇〇 m2)範圍内。 材料保護甲常規施用比率係(例如)介於〇 〇ι §至1〇〇〇 g活 性化合物/ πΛ經處理材料之間,較佳介於〇ι §至5〇 §/ 一 之間。 用於浸潰材料之殺見蟲組合物通常含有〇〇〇ι_95重量Manual ’ Brother 13 Edition ' British Crop Protection Council (2003) ° Formula M6.1 thioguanamine and its formulations are described in w〇 98/28279. Leptocin is disclosed in Agro pr0ject, pjB Publications Ltd., in mid-November. Phenyl cruzed and its formulations are described in European Patent No. EP-A1 45462 1. The smear and parax x 〇 and its formulations are described in Farm Chemicals Handbook, Vol. 88, Meister Publishing, &apos; Acetyl nitrile and its formulations are described in WO 98/28277. Methotrexate and its formulations are described in European Patent No. EP-A1 462 456. The specific gas ratio (Flupyrazofos) is described in Pesticide Science 54, 1988, pages 237-243 and U.S. Patent No. 4,822,779. Tefrop and its preparations are described in Japanese Patent No. 2002193709 and WO 01/00614. Bipro and its formulations are described in WO 98/45274 and U.S. Patent No. 63,357,357. The guanamine fibrate and its preparation are described in U.S. Patent No. 6,221,890 and Japanese Patent No. 21010907. Fluorophenol and its formulations are described in WO 03/007717 and WO 03/007718. AKD 1022 and its formulations are described in U.S. Patent No. 6,300,348. Chloranthraniliprole is described in WO 01/70671, WO 03/0155 19 and WO 05/11 δ552. The amine benzophenone derivatives of the formula M24.1 are described in WO 01/70671, WO 04/067528 and WO 05/1 18552. Butylfluorocarbon 133661.doc -152- 200917962 Esters and their formulations are described in WO 04/080180. Aminoquinazolinone compounds are described in European Patent No. A 109 7932. The M22 l, M22.2 or M22.3 quinone imine derivatives or analogues thereof and processes for their preparation are described in WO 2006/060029. The alkynyl ether compounds M22.4 and M22.5 are described, for example, in Japanese Patent No. 2006131529. Organic sulfur compounds are described in WO 2007060839. The malononitrile compound is described in 02/089579, WO 02/090320, WO 02/090321, 04/006677, WO 05/068423, WO 05/068432 and W〇05/063694 t °. The fungicidal mixed complex is selected from the following The group consisting of: acid alanines such as benalaXyi, metalaxyi, ofurace, oxadixyl; amine derivatives such as adimorpholine (aldimorph), dodine, dodemorph, fenpr〇pim〇rph, fenpropidin, guazatine, pefulang ( Iminoctadine), spir〇xamin, tridemorph, this % spray, such as pyrimethanil, mepanipyrim or eyr〇dinyi; antibiotics, for example Cycloheximide, griseofulvin, kasugamyCin, natamycin, polyoxin or streptomycin; azoles, For example, biphenyl triazole alcohol (bitertan〇i), bromoconazole, cyclopropanol (Cypr〇c〇na) Z〇ie), difenoconazole, dinic 〇na z〇le, oxiconazole 133661.doc -153- 200917962 (epoxiconazole), fenbuc〇nazole , fluquiconazole, flusilaz〇le, hexaconazole, imazalil, metconazole, myclobutanil, and sulphate. Sitting (penconazole), a ring. Place (propiconazole), propionate * (prochloraz), thiophene. Sit (pr〇thioconazole), pent. Tebuconazole, triadimefon, triadimenol, triflumizol, triticonazole, fluramide (flutriaf〇i); dicarboxymethylimine, for example Isoridine, myclozolin, procymidon, vinci〇z〇iin; dithiocarbamic acid S, such as ferbate, ferbate Nabam, maneb, mancozeb, metam, metiram, propineb, polycarbamate, Thiram, ziram, zineb 'heterocyclic compounds' such as aniiazine, benomyl, boscelid, multi-bacteria Carbendazim, carboxin, oxidized rust, Cyazofamid, dazomet, dithianon, famoxadon, fenamid 〇n), fenarimol, fuberidazole, flutlanil, furametpyr, rice dish (Isoprothiolane), destroy mines amine (mepronil), Ming-fluorophenyl 0 given alcohol (nuarimol), dilute propylbenzene ° plugs. Probenazole, pr〇qUinazid, plaque two 133661.doc -154- 200917962 (pyrifenox), pyroquinone (pyroquilon), quinoxyfen (quinoxyfen), 矽托凡 (silthiofam ), thiabendazole, thifluzamid, thioph an at e-methyl, tiadinil, tricyclic. Tricyclazole, triforine; copper fungicides, such as Bordeaux mixture, copper acetate, copper oxide, basic copper sulfate; ruthenyl phenyl derivatives, such as binapacryl , Dinocap, dinobuton, nitro-isopropyl isopropyl; phenyl 0 than the mouth 'for example, fenpiclonil or fludioxonil; sulfur; other kill Fungicides, such as S-methyl acibenzolar-S_methyl, benthiavalicarb, carpropamid, chl〇rothalonil, siaphine nano (cyflufenamid), cymoxanil, diclomezin, diclocymet, diethofencarb, edifen-phos, ethaboxam, Fenhexamid, fentin-acetate, fenoxanil, ferimzone, fluazinam, fosetyl, forsythia Aluminium, iprovalicarb, six gas stupid, mechafen〇n, bink (pencycuron), pr〇parnocarb, phthalide, 〇基特科拉夫斯(t〇i〇ci〇f〇s_methyl), pentachlorozene (quintozene), β sit Zoxamid; strobilurin, such as azulosis, azxyxytubin, dimoxystrobin, flu〇xastr〇bin, phenoxy Ester 133661.doc -155- 200917962 (kresoxim-methyl), phenoxystrobin (me_torninostrobin), ossastrobin (orsastrobin), picoxistin (pic〇xystr〇bin) or trifloxystrobin (trifloxystrobin); Acid derivatives such as captafol, captan, dichlofluanid, folpet, t〇lylfluanid; cinnamylamine and analogues' For example, dimethomorph, flumetover or flumorph. The invertebrate pests (i.e., arthropods and nematodes), the plants, the soil in which the plants are grown, or the water can be contacted with the compound of the present invention I or II or a composition containing the same by any application method known in the art. Thus, &quot;contact&quot; includes direct contact (application of the compound/composition directly to an invertebrate pest or plant _ usually applied to the leaves, stems or roots of the plant) and indirect contact (application of the compound/composition to the invertebrate) The location of the pest or plant). In addition, vertebral pests can be controlled by contacting an insecticidally effective amount of a compound or compound with a pest free, food supply, habitat, breeding ground or locus thereof. Thus, administration can be carried out before or after infection of the locus, the growing crop or the harvested crop by the pest. &quot;Location&apos; means a habitat or habitat for growing or growing pests or parasites, cultivated plants, plant propagation material (e.g., seeds), soil, area, material, or environment. In general, an effective amount of insecticide means to achieve an observable effect on growth (including necrosis, death, lag, prevention, and the effect of removing, destroying or reducing the incidence and activity of the target organism). The amount of active ingredient required. For the various compounds/compositions used in the present invention, the insecticidal effective daniel 133661.doc • 156·200917962 is changed. The insecticidally effective amount of the composition also varies depending on the insecticidal effect and duration, weather and the like. According to the main conditions (such as desired, target species, location, application model tree): and its composition can be used to protect wood materials (for example: can also be used to protect building materials, furniture, leather, fiber products B), Wires and electricity are protected from ants and/or termites. = Sacrifice and white sacrifice so that they do not cause damage to crops or humans (When the insects enter the house and public facilities). The workmanship or bismuth compound can be applied not only to the surrounding soil surface or under the floor soil to protect the wood material, but also to block objects (such as underfloor concrete, closet columns, beams, plywood, furniture, etc.) , wooden items (for example: flower board half board, etc.) and B-made products (such as enameled wire, Ethylene board, barrier material (such as benzene and ethylene), etc.). The ant control agent of the present invention can be applied to the crop or to the surrounding soil or directly to the ant nest or the like under the application of the anti-purple ant to the crop or human. It is also possible to prevent the compound of the formula w π from being applied to the place where the intended pest will occur. The compound or compound II can also be used to protect a growing plant from pest infestation or infestation by contacting the plant with a pesticidally effective amount of a compound of formula wn. Thus, "contact" includes direct contact (application of the compound/composition directly to the pest and/or plant - typically to the leaves, stems or roots of the plant) and indirect contact (8) of the composition/composition of the application of i pests and / Or ^ Location of the object. 133661.doc -157- 200917962 In the case of soil treatment or application to pest colonies or nests, the amount of active ingredient is between 0._!· g/1G() m2 (better in please Within the range of i2() g/i〇〇m2). The ratio of material protection to normal application is, for example, between 〇〇1 to 1〇〇〇g of active compound / πΛ of treated material, preferably between 〇ι § to 5〇§/ A. The insecticidal composition for impregnated materials usually contains 〇〇〇ι_95 weight

%、較佳(M-45重量%、且更佳^重量%之至少—種防護 劑及/或殺昆蟲劑。 對於誘餌組合物之用途,活性成份之含量通常佔活性化 合物之0.’重量%至15重量%、較佳佔〇〇〇1重量%至5重 量 〇/〇。 對於噴灑組合物之用途 丨土取物之含量係介於0 〇〇 i _ 重量%之間、較佳介於〇·〇1,重量%之間、且最佳介於 〇 · 01 -15重量%之間。 對於處理作物植物之用途,本發明活性成份之施用比率 可介於(Μ找4_ g/公頃之間、較佳介於25^公 頃之間、更佳在50 g至500 g/公頃之間。 在處理種子時,活性成份之施用比率—般係心山〇 kg/1〇〇kg種子,較佳係lgLkg/1〇〇kg種子,尤佳 至 200 g/100 kg種子。 現在藉由下列實例進一步詳細闡明本發明。 1.製備實例 使用以下合成實例中所述程序藉由對起始材料之適當修 133661.doc •158- 200917962 飾來製備其他式i化合物。所得化合物及物理數據列於下 表I及II中。 藉由HPLC(高效液相層析質譜法)來表徵產物。使用在4〇 C下作業之分析型RP-18管柱(來自Merck KgaA,Gemany 之Chromolith Speed ROD)來實施HPLC。使用具有(Μ體積 %三氟乙酸/水混合物及〇.丨體積%三氟乙酸之乙腈作為流動 相;流速:1.8 mL/min且注入體積:2 μ1。 實例1 3 . 1 -甲基-3 -二鼠曱基_ 1 Η- °比嗤-4-甲酸。比咬_3 -基_ 醯胺 在環境溫度下將2_5 g (12.9 mmol)存於25 mL Ν,Ν-二曱 基甲醯胺(DMF)中之1-曱基_3_三氟甲基]Η_吡唑_4_曱酸及 2·1 g (12·9 mmol) Ν,Ν’-羰基二咪唑(CDI)攪拌i小時,之後 添加1.2 g (12.9 mmol) 3-胺基吡啶。搜拌三天後使溶劑蒸 發’將殘餘物溶於二氣甲烷中,用NaHC03與水之飽和溶 液洗滌兩次。蒸發經合併有機相且藉由急驟管柱層析法 (一氧化石夕,使用二氯甲烧/甲醇=95/5)純化粗產物來獲得 1·33 g (48%)標題化合物。 實例29 : 1-甲基-3-三氟甲基-1H-吡唑-4-甲酸甲基-吡啶_3_ 基-酿胺 在環境溫度下攪拌1.0 g (3.7 mmol)來自實例13且存於1〇 mL四氫。夫喃(thf)中之1 -曱基-3-三氟甲基_丨H-吼ϋ坐_4_曱酸 吡啶-3-基-醯胺及3.7 g (11·! mm〇1)碳酸铯且將79〇 mg (5 ’55 mmol)蛾曱烷添加至混合物中。攪拌兩天後過濾懸浮 液’使溶劑蒸發且藉由急驟管柱層析法(二氧化矽,使用 I33661.doc -159- 200917962 環己烷/乙酸乙酯)來獲得327 mg (31%)純化粗產物曱基化 醯胺。 表I :式I化合物%, preferably (M-45% by weight, and more preferably ^% by weight of at least one type of protective agent and/or insecticide. For the use of the bait composition, the active ingredient is usually present in an amount of 0.' weight of the active compound. % to 15% by weight, preferably 〇〇〇1% by weight to 5% by weight 〇/〇. For the application of the spray composition, the content of the ramie is between 0 〇〇i _% by weight, preferably between 〇·〇1, between % by weight, and optimally between 〇· 01 -15% by weight. For the treatment of crop plants, the application rate of the active ingredient of the present invention may be between (Μ 4 g/ha) Preferably, it is between 25 and 5 hectares, more preferably between 50 g and 500 g/ha. When the seed is treated, the application rate of the active ingredient is generally 系 心 〇 kg/1 〇〇 kg of seed, preferably lgLkg / 1 〇〇 kg seeds, particularly preferably 200 g / 100 kg seeds. The invention will now be further illustrated in detail by the following examples: 1. Preparation Examples The procedures described in the following synthesis examples were used by appropriate starting materials Repair 133661.doc •158- 200917962 to prepare other compounds of formula i. The data are listed in Tables I and II below. The product was characterized by HPLC (High Performance Liquid Chromatography Mass Spectrometry) using an analytical RP-18 column operating at 4 ° C (Chromolith from Merck KgaA, Gemany) Speed ROD) was carried out to carry out HPLC using acetonitrile having (Μ volume % trifluoroacetic acid / water mixture and 〇 丨 volume % trifluoroacetic acid as mobile phase; flow rate: 1.8 mL / min and injection volume: 2 μ1. Example 1 3 1 -Methyl-3 -dimurium _ 1 Η- ° than 嗤-4-carboxylic acid. 2 _5 g (12.9 mmol) in 25 mL 环境 at ambient temperature. 1-mercapto-3-3-trifluoromethyl]indole-pyrazole_4_decanoic acid and 2·1 g (12·9 mmol) in Ν-dimercaptocaramine (DMF) Ν,Ν'- The carbonyl diimidazole (CDI) was stirred for 1 hour, after which 1.2 g (12.9 mmol) of 3-aminopyridine was added. After three days of mixing, the solvent was evaporated. The residue was dissolved in di-methane, and saturated solution of NaHC03 and water was used. Wash twice. Evaporate the combined organic phases and purify the crude product by flash column chromatography (e.g., EtOAc, m. Compound. Example 29: 1-A 3-trifluoromethyl-1H-pyrazole-4-carboxylic acid methyl-pyridine-3-yl-bristamine was stirred at ambient temperature 1.0 g (3.7 mmol) from Example 13 and stored in 1 mL of tetrahydrogen. 1 - mercapto-3-trifluoromethyl 丨 H-吼ϋ sitting _4_pyridylpyridin-3-yl-decylamine and 3.7 g (11·! mm〇1) cesium carbonate And 79 〇 mg (5 '55 mmol) mothane was added to the mixture. After stirring for two days, the suspension was filtered. 'The solvent was evaporated and purified by flash column chromatography (c.c., using I33661.doc - 159 - 200917962 hexane/ethyl acetate) to obtain 327 mg (31%). The crude product is guanidinated with guanamine. Table I: Compounds of formula I

AA

(I) 實例 A R1 R2 R3 物理-化學數據 r.t. [mini 1 卜甲基-1H-«比&quot;坐-3-基 Η Η Η n.d. 2 1-GU-—氣笨氧基甲某1H_吡嗤·3·基 Η Η Η 2.461 3 2,5-_甲基-2Η·σΛ〇坐-3-基 Η Η Η 1.320 4 4-氣-2,5-二甲某-2Η-吡唑-3-基 卜Η Η Η 1.543 5 5-氣-1-甲基-1Η·吡唑-3-基 Η Η Η 1.499 6 1-甲基-5-三氟甲基_ΐΗ-〇比唑-3-基 Η Η Η 1.779 7 4-氣-ί·曱基-1Η·吡唑-3-基 Η Η Η 1.353 8 1-甲基笨基-1H-吡唑-3-基 Η Η Η 2.124 9 2-甲基-5-苯基-2H-t坐-3-基 Η Η Η 2.193 10 1,5-二甲基_1沁吡唑-3-某 Η Η Η 1.311 11 2-甲基三氟甲基-2H-吡唑-3-基 Η Η Η 1.954 12 2-曱基-2H-吡唑-3-基 Η Η Η 1.125 13 1-曱基-3·三氟曱基-1H·。比嗤斗基 Η Η Η 1.548 14 3-二氟曱基-1-曱基-1H-吡唑-4-基 Η Η Η 1.295 15 1-(6-氯°比咬-2·基)_5_三氣曱基-iH-t坐-4·基 Η Η Η 2.273 16 1-节基-5-三1曱基-旧-。比〇坐-4-基 Η Η Η 2.290 17 1-乙基-3-三氟甲基-11^-〇比。坐-4-基 Η Η Η 1.771 1-乙基-5-三氟曱基-1Η-η比吐-4-基 Η Η Η 1.704 19 1-稀丙基-3-三氣曱基-111-〇比11坐-4-基 Η Η Η 2.187 20 5-二氟甲基-1-甲基-1Η-吡唑-4-基 ’ Η Η Η 1.588 21 5-氰基-1 -(2,4-二氯苯基)-1 Η-°比啥·4-基 Η Η Η 2.475 22 5-三氟甲基-1-(4-氣苯基)-1Η-吡唑-4-基 Η Η Η 2.517 23 5-三氟甲基-1-苯基-1Η-。比唑-4-基 卜Η Η Η 2.185 24 1-(2,4-二氣苯基)-5-二氟曱基-出-°比嗤-4·基 Η Η Η 2.587 25 1-(4·敗苯基)-5-甲基·1Η-°比。坐-4-基 Η Η Η 1.834 26 1-(2,2,2-三氟乙基)-5-二敗甲基比。坐_ 4-基 Η Η Η 1.980 27 5-氯-1-甲基-3-三氟甲基-1Η-吼唑-4-基—' Η Η Η 1.651 28 1-甲基-3-三氟曱基-m-'比唑-4-基 苄基 Η Η 2.457 133661.doc -160· 200917962 實例 A R1 R2 R3 物理-化學數據 r.t. [min] 29 1-曱基-3-三氟甲基-1 Η-吡唑-4-基 ch3 Η Η 1.504 30 1 -第三丁基-5-三氟曱基-1Η-吡唑-4-基 Η Η Η 2.197 31 1-(4-硝基苯基)-5-三氟甲基-1Η-&quot;比唑-4-基 Η Η Η 2.269 32 1-(5-氣吡啶-2-基)-5-三氟曱基-1H-吡唑-4-基 Η Η Η 2.339 33 1-曱基-3-三氟曱基-1H-吡唑-4-基 Η Η ch3 1.793 34 1-曱基-3-三氟曱基-1H-吡唑-4-基 Η Η Cl 2.444 35 5-二氟曱基-1-曱基-1H-吡唑-4-基 c2h5 Η Η 1.645 36 5-二氟甲基-1-甲基-1H-吡唑-4-基 ch3 Η Η 1.487 37 1-曱基-3-三氟甲基-1H-吡唑-4-基 Η Η cf3 2.844 38 1-曱基-3-三氟甲基-1H-吡唑-4-基 Η Η F 2.194 39 卜異丙基-3-三氟曱基-1H-吼唑-4-基 Η Η Η 2.041 40 1-異丁基-3-三氟曱基-1H-吡唑-4-基 Η Η Η 2.271 41 1 -甲基-3-三氟甲基-1H-吡唑-4-基 Η ch3 Η 1.597 42 5-氣-1,3-二甲基-1H-吡唑-4-基 Η Η Η 1.385 43 1-丙基-3-三氟曱基-1H-吡唑-4-基 Η Η Η 2.040 44 1-甲基-3-乙氧基-1H-吡唑-4-基 Η Η Η 1.550 45 1-丙基-5-三氟曱基-1H-吡唑-4-基 Η Η Η 2.101 46 5-三氟曱基-1H-吡唑-4-基 Η Η Η 1.410 47 3-環丙基-1-曱基-1H-吡唑-4-基 Η Η Η 1.491 48 1 -(2,2,2-三氟乙基)-5-三氟曱基-1 H-吡唑-4-基 ch3 Η Η 2.032 49 1-(2,2,2-三氟乙基)-5-三氟甲基-1H-。比唑- 4-基 C2H5 Η Η 2.281 50 1-(2,2,2-三氟乙基)-5-三氟曱基-1H-。比唑-4-基 異丁 基 Η Η 2.767 51 1 -曱基-3-三氟曱基-1 H-°比唑-4-基 Η C1 Η 1.868 52 1 -甲基-3-三氟甲基-1H-吼唑-4-基 Η OCH 3 Η 1.652 53 3-甲氧基-1-甲基-1H-吡唑-4-基 Η Η Η 1.333 54 5-溴-2-(3-氣吡啶-2-基)-2H-吡唑-3-基 Η Η 1,92 55 2-(3-氣吡啶-2-基)-5-三氟曱基-2Η-»比唑-3-基 Η Η Η 2.283 56 3-三氟曱基-1-(4-氣苯基)-1Η-«比唑-4-基 Η Η Η 2.548 57 H4-曱氧基苯基)-5-曱基-1Η-»比唑-4-基 Η Η Η 2.005 58 5-笨基-1H-吡唑-4-基 Η Η Η 1.504 59 1-乙基-5-曱基-1H-吡唑-4-基 Η Η Η 1.426 60 1-甲基-5-苯基-1H-吡唑-4-基 Η Η Η 1.751 61 1,3-二甲基-11^-吡唑-4-基 Η Η Η 1.219 62 2-曱基-5-第三丁基-2H-吡唑-3-基 Η Η Η 1.78 63 2-曱基-4-氣-2H-吡唑-3-基 Η Η Η 1.49 64 2-(3-氣。比啶-3-基)-5-三氟曱基-2H-吡唑-3-基 Η Η Η 2.28 65 4-異丙基-1-甲基-1H-吡唑-3-基 Η Η Η 1.81 66 5-異丙基-2-曱基-2H-吡唑-3-基 Η Η Η 1.56 • 16】- 133661.doc 200917962 實例 A R1 R2 R3 物理-化學數據 r.t. [min] 67 5-乙基-2-曱基-2H-吡唑-3-基 Η Η Η 1.53 68 4,5-二曱基-2-甲基-2H-吡唑-3-基 Η Η Η 1.42 69 2-甲基-5-正丙基-2H-吡唑-3-基 Η Η Η 1.76 r.t.保留時間 n. d.未測定 表II :式I.A1化合物(I) Example A R1 R2 R3 Physico-chemical data rt [mini 1 卜 methyl-1H-« ratio &quot; sit-3-yl Η Η nd nd 2 1-GU--gas phenoxy A certain 1H_pyridinium 3.·············· Η Η Η Η 1.543 5 5-Ga-1-methyl-1 Η·pyrazol-3-ylindole Η Η 1.499 6 1-Methyl-5-trifluoromethyl ΐΗ-indoleazole-3-yl hydrazine Η Η 1.779 7 4-气-ί·曱基-1Η·pyrazole-3-ylindole Η 353 1.353 8 1-methylphenyl-1H-pyrazole-3-ylindole Η Η 2.124 9 2-methyl -5-phenyl-2H-t--3-ylindole Η Η 2.193 10 1,5-dimethyl-1 oxapyrazole-3- Η Η Η 1.311 11 2-methyltrifluoromethyl-2H -pyrazol-3-ylindole Η 954 1.954 12 2-mercapto-2H-pyrazole-3-ylindole Η 1.125 13 1-mercapto-3·trifluoromethyl-1H.比 嗤 Η Η 548 548 1.548 14 3-Difluorodecyl-1-indolyl-1H-pyrazole-4-ylindole Η 295 1.295 15 1-(6-Chloro ratio bite-2·base)_5_ Tri-gas sulfhydryl-iH-t sits -4 Η Η Η 273 2.273 16 1-member base-5-three 1 曱 base-old-. 〇 -4- -4- Η Η Η Η 2.290 17 1-ethyl-3-trifluoromethyl-11^-〇 ratio. -4--4-基Η Η Η 1.771 1-ethyl-5-trifluoromethyl-1Η-η ratio 吐-4-基Η Η 704 1.704 19 1-Lactyl-3-trisyl fluorenyl-111- 〇 11 11 -4- Η Η Η 187 2.187 20 5-Difluoromethyl-1-methyl-1 Η-pyrazole-4-yl' Η Η Η 1.588 21 5-cyano-1 - (2,4 -Dichlorophenyl)-1 Η-° 比啥·4-基Η Η Η 2.475 22 5-Trifluoromethyl-1-(4-phenylphenyl)-1Η-pyrazole-4-ylindole Η Η 2.517 23 5-Trifluoromethyl-1-phenyl-1Η-.比 -4- -4- 基 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 185 · Deficient phenyl)-5-methyl·1Η-° ratio. Sodium-4-yl Η Η Η 1.834 26 1-(2,2,2-trifluoroethyl)-5-dioxmethyl ratio. _ 4-基Η Η Η 1.980 27 5-Chloro-1-methyl-3-trifluoromethyl-1 Η-oxazol-4-yl-' Η Η Η 1.651 28 1-methyl-3-trifluoro Mercapto-m-'bazol-4-ylbenzyl hydrazine 457 2.457 133661.doc -160· 200917962 Example A R1 R2 R3 Physical-chemical data rt [min] 29 1-mercapto-3-trifluoromethyl- 1 Η-pyrazol-4-yl ch3 Η Η 1.504 30 1 -T-butyl-5-trifluoromethyl-1Η-pyrazole-4-ylindole Η 197 2.197 31 1-(4-nitrophenyl )-5-trifluoromethyl-1Η-&quot;Bizozol-4-ylindole Η 269 2.269 32 1-(5-apyridin-2-yl)-5-trifluorodecyl-1H-pyrazole-4 - Η Η Η 339 2.339 33 1-mercapto-3-trifluoromethyl-1H-pyrazole-4-ylindole Η ch3 1.793 34 1-mercapto-3-trifluoromethyl-1H-pyrazole-4 -based ΗCl 2.444 35 5-difluorodecyl-1-indenyl-1H-pyrazol-4-yl c2h5 Η Η 1.645 36 5-difluoromethyl-1-methyl-1H-pyrazole-4 -based ch3 Η Η 1.487 37 1-mercapto-3-trifluoromethyl-1H-pyrazole-4-ylindole cf cf3 2.844 38 1-mercapto-3-trifluoromethyl-1H-pyrazole-4 -based Η F 2.194 39 isopropyl-3-trifluoromethyl-1H-indazole-4-ylindole Η Η 2.041 40 1-isobutyl-3-trifluoromethyl-1H-pyrazole- 4-基Η Η Η 2.271 41 1-methyl-3-trifluoromethyl-1H-pyrazole-4-ylindole ch3 Η 1.597 42 5-Gas-1,3-dimethyl-1H-pyrazole-4-ylindole Η Η 1.385 43 1-propyl-3-trifluoromethyl-1H-pyrazole-4-ylindole Η Η 2.040 44 1-methyl-3-ethoxy-1H-pyrazole-4-ylindole Η Η 1.550 45 1 -propyl-5-trifluoromethyl-1H-pyrazole-4-ylindole Η Η 2.101 46 5-trifluoromethyl-1H-pyrazole-4-ylindole Η Η 1.410 47 3-cyclopropyl- 1-mercapto-1H-pyrazole-4-ylindole Η 491 1.491 48 1 -(2,2,2-trifluoroethyl)-5-trifluorodecyl-1 H-pyrazole-4-yl ch3 Η Η 2.032 49 1-(2,2,2-Trifluoroethyl)-5-trifluoromethyl-1H-. Bisazo-4-yl C2H5 Η Η 2.281 50 1-(2,2,2-trifluoroethyl)-5-trifluoromethyl-1H-. Biazol-4-ylisobutylphosphonium 767 2.767 51 1 -mercapto-3-trifluoromethyl-1 H-°boxazol-4-ylindole C1 Η 1.868 52 1 -methyl-3-trifluoromethyl -1H-carbazole-4-ylindole OCH 3 Η 1.652 53 3-methoxy-1-methyl-1H-pyrazole-4-ylindole Η 333 1.333 54 5-bromo-2-(3- gas Pyridin-2-yl)-2H-pyrazol-3-ylindole Η 1,92 55 2-(3-Apyridin-2-yl)-5-trifluoromethyl-2Η-»Bizozol-3-yl 283 Η Η 2.283 56 3-Trifluorodecyl-1-(4-phenylphenyl)-1Η-«bizozol-4-ylindole Η 548 2.548 57 H4-decyloxyphenyl)-5-fluorenyl- 1Η-»Bizozol-4-ylindole Η Η 2.005 58 5-phenyl-1H-pyrazole-4-ylindole Η 504 1.504 59 1-ethyl-5-mercapto-1H-pyrazol-4-yl 426 Η Η 1.426 60 1-Methyl-5-phenyl-1H-pyrazole-4-ylindole Η 751 1.751 61 1,3-Dimethyl-11^-pyrazole-4-ylindole Η Η 1.219 62 2-mercapto-5-t-butyl-2H-pyrazole-3-ylindole Η 78 1.78 63 2-mercapto-4-pyrene-2H-pyrazole-3-ylindole Η Η 1.49 64 2-( 3-oxi.pyridin-3-yl)-5-trifluoromethyl-2H-pyrazole-3-ylindole Η 2.28 65 4-isopropyl-1-methyl-1H-pyrazole-3-基Η Η Η 1.81 66 5-isopropyl-2-mercapto-2H-pyrazole-3-ylindole Η Η 1.56 • 16]- 133661.do c 200917962 Example A R1 R2 R3 Physical-chemical data rt [min] 67 5-ethyl-2-mercapto-2H-pyrazole-3-ylindole Η Η 1.53 68 4,5-dimercapto-2-yl -2-2H-pyrazol-3-ylindole Η Η 1.42 69 2-methyl-5-n-propyl-2H-pyrazole-3-ylindole Η 76 1.76 rt retention time nd not determined Table II: Formula I. A1 compound

Ex. R41 R51 R61 R1 R2 R3 r.t. [min] ΐ m.p. [°C] 70 H ch3 ch3 Η Η Η 1.27 n.d. 71 苯基 Η ch3 Η Η Η 1.80 n.d. 72 ch3 Η c2h5 Η Η Η 1.47 n.d. 73 H cf3 4-氯苯基 Η Η Η 2.59 n.d. 74 苯基 Η Η Η Η Η 1.50 n.d. 75 ch3 Η 4-曱氧基-苯基 Η Η Η 2.01 n.d. 76 4-氟-苯基 Η Η Η Η Η 1.57 n.d. 77 2-11 塞吩基 Η Η Η Η Η 1.47 n.d. 78 F cf3 ch3 Η Η Η 1.63 n.d. 79 正丙基 Η 4-氣苯基 Η Η Η 2.53 n.d. 80 chf2 Η 1-曱基-1,3,4-三 嗓-2-基 Η Η Η n.d· 130 81 Η Η 4-氣苄基 Η Η Η n.d. 218 82 Η Η 苄基 Η Η Η n.d. 165 83 Cl Η ch3 Η Η Η n.d. 186 84 Η ch3 苯基 Η Η Η 2.08 n.d. 85 chf2 Η 4-(三氟曱基)苯 基 Η Η Η 2.75 n.d 86 chf2 Η 4-氯苯基 Η Η Η 2.55 n.d. 87 Η Η Η Η Η Η 0.54 n.d. 88 chf2 Η 4-(曱基-磺醯 基)-苯基 Η Η Η 1.89 n.d. 89 環丙基 Η ch3 Η Η Η 1.41 n.d. 90 異丙基 Η ch3 Η Η Η 1.65 n.d. 133661.doc -162- 200917962Ex. R41 R51 R61 R1 R2 R3 rt [min] ΐ mp [°C] 70 H ch3 ch3 Η Η Η 1.27 nd 71 phenyl Η ch3 Η Η Η 1.80 nd 72 ch3 Η c2h5 Η Η Η 1.47 nd 73 H cf3 4 -chlorophenyl hydrazine Η 59 2.59 nd 74 phenyl hydrazine Η Η Η Η 1.50 nd 75 ch3 Η 4-曱 oxy-phenyl Η Η Η 2.01 nd 76 4-fluoro-phenyl Η Η Η Η Η 1.57 nd 77 2-11 塞 Η Η 47 47 F Η 47 1.47 nd 78 F cf3 ch3 Η Η Η 1.63 nd 79 n-propyl fluorene 4-phenylphenyl hydrazine Η Η 2.53 nd 80 chf2 Η 1-meryl-1,3,4 -三嗓-2-基Η Η Η nd· 130 81 Η Η 4-gasbenzyl Η Η nd nd 218 82 Η 苄 benzyl Η Η nd nd 165 83 Cl Η ch3 Η Η nd nd 186 84 Η ch3 phenyl Η Η Η 2.08 nd 85 chf2 Η 4-(Trifluoromethyl)phenyl Η Η Η 2.75 nd 86 chf2 Η 4-chlorophenyl Η Η Η 2.55 nd 87 Η Η Η Η Η Η 0.54 nd 88 chf2 Η 4- (曱-sulfonyl)-phenylhydrazine Η Η 1.89 nd 89 cyclopropyl hydrazine ch3 Η Η Η 1.41 nd 90 isopropyl hydrazine ch3 Η Η Η 1.65 nd 133661.doc -162- 200917962

Ex. R41 R51 R61 R1 R2 R3 r.t. [min]; m.p. [°C] 91 2-甲基-丙基 H ch3 Η Η Η 2.71 ; n.d. 92 chf2 H 4-(七氣-異丙 基)-苯基 Η Η Η 3.12 ; n.d. 93 chf2 H 4-(三氟-甲硫 基)-苯基 Η Η Η 2.94 ; n.d. 94 chf2 H 4-氟苯基 Η Η Η 2.39 ; n.d. 95 chf2 H 4-(三氟-甲氧 基)-苯基 Η Η Η 2.73 ; n.d. 96 c(=o)nh2 H ch3 Η Η Η n.d. ; 230 97 H H 異丙基 Η Η Η n.d. ; 174 98 H H 2-曱基丙基 Η Η Η n.d. ; 143 99 H H 2,2-二氟-乙基 Η Η Η n.d. ; 152 100 H cf3 ch3 Η Η Η 1.69 ; n.d. (作為N-氧化 物) 101 chf2 H 2,6-二氣-4-(三 氟-曱基)苯基 Η Η Η 2.91 n.d. 102 H H 乙基 Η Η Η n.d. 126 103 H H 2,2,2-三氟乙基 Η Η Η n.d. 191 104 H cf3 4-(三氟-甲基)-噻唑啉-2-基 Η Η Η n.d. 194 105 H H 0比°定-2-基 Η Η Η n.d. 244 106 H H 苯基 Η Η Η n.d. 241 107 H H ch3 Η Η Η n.d. 180 108 H H 正丙基 Η Η Η n.d. 119 109 cf3 H ch3 Η Η Η 1.51 n.d. 110 H ochf2 ch3 Η Η Η 1.43 n.d. 111 H cf3 苄基 Η Η Η 2.34 n.d. 112 H cf2ci ch3 Η Η Η 1.69 n.d. 113 H H 4-氟苯基 Η Η Η n.d. 235 114 H H (4-硝基-°比。坐-1 -基)-曱基 Η Η Η n.d. 227 115 ch3 H 1-曱基-1,3,4-三 。秦-2-基 Η Η Η n.d. ; 206 116 ch3 H 噻唑-2-基 Η Η Η n.d. ; 205 117 chf2 H 4-(三氟-曱基)噻 唑-2-基 Η Η Η n.d. ; 171 118 ch3 H 4-(三氟曱基)噻 唑-2-基 Η Η Η n.d· ; 240 119 H H 環丙基 Η Η Η n.d. ; 145 120 異丙基 H 苯基 Η Η Η 2.32 i n.d. 133661.doc -163 - 200917962Ex. R41 R51 R61 R1 R2 R3 rt [min]; mp [°C] 91 2-methyl-propyl H ch3 Η Η Η 2.71 ; nd 92 chf2 H 4-(seven-isopropyl)-phenyl Η ch Η 3.12 ; nd 93 chf2 H 4-(trifluoro-methylthio)-phenylhydrazine Η Η 2.94 ; nd 94 chf2 H 4-fluorophenyl Η Η Η 2.39 ; nd 95 chf2 H 4-(trifluoro -methoxy)-phenylindole Η 73 2.73 ; nd 96 c(=o)nh2 H ch3 Η Η Η nd ; 230 97 HH isopropyl hydrazide Η nd ; 174 98 HH 2-mercaptopropyl hydrazine 143 nd ; 143 99 HH 2,2-difluoro-ethyl Η Η nd nd ; 152 100 H cf3 ch3 Η Η Η 1.69 ; nd (as N-oxide) 101 chf2 H 2,6-diox-4- (trifluoro-indenyl)phenylindole Η Η 2.91 nd 102 HH ethyl Η Η nd nd 126 103 HH 2,2,2-trifluoroethyl Η Η nd 191 104 H cf3 4-(trifluoro-A ))-thiazolin-2-ylindole Η Η nd 194 105 HH 0 ratio °-2-ylindene Η nd nd 244 106 HH phenyl Η Η nd nd 241 107 HH ch3 Η Η Η nd 180 108 HH positive Η Η nd nd 119 109 cf3 H ch3 Η Η Η 1.51 nd 110 H ochf2 ch3 Η Η Η 1.43 nd 111 H cf3 benzyl 34 Η Η 2.34 nd 112 H cf2ci ch3 Η Η Η 1.69 nd 113 HH 4-fluorophenyl Η Η nd nd 235 114 HH (4-nitro-° ratio. sit-1 -yl)-fluorenyl Η Η nd 227 115 ch3 H 1-mercapto-1,3,4-tri. Qin-2-ylindole Η 206 nd; 206 116 ch3 H thiazol-2-ylindole Η Η nd ; 205 117 chf2 H 4-(trifluoro-indenyl)thiazol-2-ylindole Η Η nd ; 171 118 ch3 H 4-(Trifluoromethyl)thiazol-2-ylindole Η nd· ; 240 119 HH cyclopropyl Η Η nd nd ; 145 120 isopropyl H phenyl Η Η Η 2.32 i nd 133661.doc -163 - 200917962

Ex. R41 r51 R61 R1 R2 R3 r,t. [min]; m.p. [°C] 121 ch3 H 4,5-二甲基-噻 唑-2-基 Η Η Η n.d. ; 235 122 chf2 H 4,5-二曱基-噻 唑-2-基 Η Η Η n.d. ; 182 123 Cl H 苯基 Η Η Η n.d. ; 171 124 I H 4-氟苯基 Η Η Η n.d. ; 188 125 H 2·氟-乙 基 ch3 Η Η Η 1.22 ; n.d. 126 H cf3 ch3 環丙基-曱基 Η Η 2.13 ; n.d. 127 H cf3 ch3 乙基 Η Η 1.73 ; n.d. 128 chf2 H 3-甲基-3H-1,3,4-三嗪-2-基 Η Η Η 1.18 ; n.d. 129 H cf3 ch3 正丙基 Η Η 2.06 ; n.d. 130 H cf3 ch3 異丙基 Η Η 2.00 ; n.d. 131 H cf3 ch3 (1-曱基-3-(三氟-曱基)-°比唑-4-基) 羰基 Η Η 186 ; n.d. 132 H cf3 ch3 第三丁氧基-羰 基 Η Η n.d. n.d. 133 H cf3 ch3 第三丁基-羰基 Η Η 2.83 n.d. 134 H cf3 ch3 乙醯基 Η Η n.d. 143 135 chf2 H 2,4-二氟苯基 Η Η Η 2.38 n.d. 136 H cf3 ch3 曱苯磺醯基 Η Η 2.98 n.d. 137 chf2 H 3,5-二氣苯基 Η Η Η 2.77 n.d. 138 chf2 H 4-曱苯基 Η Η Η 2.43 n.d. 139 H cf3 ch3 ch2-cn Η Η 1.88 n.d. 140 H H 正庚基 Η Η Η 2.63 n.d. 141 H cf3 ch3 2-丙炔基 Η Η 1.89 n.d. 142 ch3 H 4-氣苯基 Η Η Η 2.26 n.d. 143 乙基 H 4-氯苯基 Η Η Η 2.42 n.d· 144 乙基 H 4-硝基苯基 Η Η Η 2.26 n.d. 145 乙基 H 4-(三氟-甲基)苯 基 Η Η Η 2.69 n.d. 146 乙基 H 4-氟苯基 Η Η Η 2.26 n.d. 147 chf2 H 3-(三氟-甲基) 苯基 Η Η Η 2.61 n.d. 148 chf2 H 2-氣苯基 Η Η Η 2.24 n.d. 149 chf2 H 2-(三氟-曱基) 苯基 Η Η Η 2.38 n.d. 150 chf2 H 2-曱氧基-苯基 Η Η Η 2.12 n.d. 151 chf2 H 3-氣-4-氟苯基 Η Η Η 2.54 n.d. 152 chf2 H 4-第三丁基苯基 Η Η Η 2.95 n.d. 133661.doc -164- 200917962Ex. R41 r51 R61 R1 R2 R3 r,t. [min]; mp [°C] 121 ch3 H 4,5-dimethyl-thiazol-2-ylindole Η Η nd ; 235 122 chf2 H 4,5- Didecyl-thiazol-2-ylindole Η nd ; 182 123 Cl H phenyl hydrazine Η nd ; 171 124 IH 4-fluorophenyl Η Η Η nd ; 188 125 H 2 · fluoro-ethyl ch3 Η Η Η 1.22 ; nd 126 H cf3 ch3 cyclopropyl-fluorenyl hydrazine 2.13 ; nd 127 H cf3 ch3 ethyl hydrazine Η 1.73 ; nd 128 chf2 H 3-methyl-3H-1,3,4-triazine-2 - Η Η Η 1.18 ; nd 129 H cf3 ch3 n-propyl hydrazine Η 2.06 ; nd 130 H cf3 ch3 isopropyl hydrazine Η 2.00 ; nd 131 H cf3 ch3 (1-mercapto-3-(trifluoro-fluorenyl) )-°bizozol-4-yl)carbonyl Η 186 186 ; nd 132 H cf3 ch3 third butoxy-carbonyl Η nd ndnd 133 H cf3 ch3 third butyl-carbonyl Η Η 2.83 nd 134 H cf3 ch3 醯基Η nd 143 135 chf2 H 2,4-DifluorophenylΗ Η Η 2.38 nd 136 H cf3 ch3 Benzene sulfonyl hydrazine Η 2.98 nd 137 chf2 H 3,5-diphenylphenyl Η Η 77 2.77 nd 138 chf2 H 4-曱phenylΗ Η Η 2.43 nd 139 H cf3 ch3 ch2-cn Η Η 1.88 Nd 140 HH n-heptyl Η Η Η 2.63 nd 141 H cf3 ch3 2-propynyl Η Η 1.89 nd 142 ch3 H 4-Phenylphenyl Η Η Η 2.26 nd 143 Ethyl H 4-chlorophenyl Η Η Η 2.42 Nd· 144 ethyl H 4-nitrophenyl hydrazine Η 2.26 nd 145 ethyl H 4-(trifluoro-methyl)phenyl hydrazine Η 2.69 nd 146 ethyl H 4-fluorophenyl Η Η Η 2.26 Nd 147 chf2 H 3-(trifluoro-methyl)phenyl Η Η Η 2.61 nd 148 chf2 H 2-phenylphenyl Η Η 24 2.24 nd 149 chf2 H 2-(trifluoro-indenyl)phenyl Η Η Η 2.38 nd 150 chf2 H 2-decyloxy-phenylindole Η Η 2.12 nd 151 chf2 H 3-vapor-4-fluorophenyl Η Η Η 2.54 nd 152 chf2 H 4-tert-butylphenyl Η Η Η 2.95 Nd 133661.doc -164- 200917962

Ex. R41 R51 R61 R1 R2 R3 r,t. [min]; m.p. [°C】 153 chf2 H 3-硝基苯基 Η H H 2.25 n.d. 154 chf2 H 3,4-二氣-苯基 Η H H 2.75 n.d. 155 chf2 H 2,4-二氣-苯基 Η H H 2.62 n.d. 156 chf2 H 2-曱苯基 Η H H 2.34 n.d. 157 chf2 H 3-氣苯基 Η H H 2.46 n.d. 158 chf2 H 3-曱苯基 Η H H 2.42 n.d. 159 chf2 H 4-氯-2-氟苯基 Η H H 2.57 n.d. 160 chf2 H 2,4,6-三氯-苯基 Η H H 2.79 n.d. 161 chf2 H 2,3,4-三氯-笨基 Η H H 2.85 n.d. 162 chf2 H 2,6-二氟-苯基 Η H H 2.29 n.d. 163 H cf3 ch3 乙氧基-羰基 H H n.d· ; 104 164 H cf3 ch3 乙氧基-曱基 H H 2.19 ; n.d. 165 ch3 H 4-氟苯基 Η H H 2.17 ; n.d.; (作為N-氧化 物) 166 ch3 H 4-(三氟-甲基) 笨基 Η H H 2.50 ; n.d. 167 chf2 H ch3 Η H H n.d. ; 172 ;(作 為鹽酸鹽) 168 cf3 H 2,2,2·三氟-乙基 乙醯基 H H 2.52 ; n.d. 169 cf3 H 2,2,2-三氟-乙基 ch3 H H n.d. ; 131 ;(作 為N-氧化物) 170 H chf2 ch3 Η H H 1.67 ; n.d.; (作為N-氧化 物) 171 H chf2 4-硝基苯基 Η H H 2.46 n.d. 172 ch3 H 2,2,2-二氣-乙基 Η H H 1.65 n.d. 173 ch3 H 2,2,2-三氟-乙基 ch3 H H 1.79 n.d. 174 cf3 H ch3 ch3 H H 1.44 n.d. 175 chf2 H 2,2,2-三氟-乙基 Η H H 2.07 n.d. 176 chf2 H 2,2,2-三氟-乙基 ch3 H H 1.82 n.d. 177 H H ch3 ch3 H H 0.85 n.d. 178 ch3 H ch3 ch3 H H 0.99 n.d. 179 ch3 H ch3 Η H H 1.32 n.d. 180 ch3 H 乙基 ch3 H H 1.22 n.d. 181 H chf2 乙基 Η H H 2.00 n.d. 182 H chf2 乙基 ch3 H H 1.39 n.d. 183 H cf3 乙基 ch3 H H 1.77 n.d. 184 乙基 H 乙基 H H H 1.59 n.d. 185 乙基 H 乙基 ch3 H H 1.49 n.d. 186 cf3 H 乙基 ch3 H H 1.89 n.d. 187 H H 乙基 ch3 H H 1.11 n.d. 133661.doc -165 - 200917962Ex. R41 R51 R61 R1 R2 R3 r,t. [min]; mp [°C] 153 chf2 H 3-nitrophenylhydrazine HH 2.25 nd 154 chf2 H 3,4-digas-phenylhydrazine HH 2.75 nd 155 chf2 H 2,4-diqi-phenylhydrazine HH 2.62 nd 156 chf2 H 2-indole hydrazine HH 2.34 nd 157 chf2 H 3-phenylphenyl hydrazine HH 2.46 nd 158 chf2 H 3-hydrazino hydrazine HH 2.42 nd 159 chf2 H 4-chloro-2-fluorophenyl hydrazine HH 2.57 nd 160 chf2 H 2,4,6-trichloro-phenylhydrazine HH 2.79 nd 161 chf2 H 2,3,4-trichloro-stupyl Η HH 2.85 nd 162 chf2 H 2,6-difluoro-phenylhydrazine HH 2.29 nd 163 H cf3 ch3 ethoxy-carbonyl HH nd· ; 104 164 H cf3 ch3 ethoxy-fluorenyl HH 2.19 ; nd 165 ch3 H 4-fluorophenylhydrazine HH 2.17 ; nd; (as N-oxide) 166 ch3 H 4-(trifluoro-methyl) stupyl hydrazine HH 2.50 ; nd 167 chf2 H ch3 Η HH nd ; 172 ; Hydrochloride) 168 cf3 H 2,2,2·trifluoro-ethylethylhydrazine HH 2.52 ; nd 169 cf3 H 2,2,2-trifluoro-ethyl ch3 HH nd ; 131 ; (as N-oxidation 170 H chf2 ch3 Η HH 1.67 ; nd; (as N-oxide) 171 H chf2 4-nitrobenzene Η HH 2.46 nd 172 ch3 H 2,2,2-digas-ethyl hydrazine HH 1.65 nd 173 ch3 H 2,2,2-trifluoro-ethylch3 HH 1.79 nd 174 cf3 H ch3 ch3 HH 1.44 nd 175 chf2 H 2,2,2-trifluoro-ethylhydrazine HH 2.07 nd 176 chf2 H 2,2,2-trifluoro-ethylch3 HH 1.82 nd 177 HH ch3 ch3 HH 0.85 nd 178 ch3 H ch3 ch3 HH 0.99 nd 179 Ch3 H ch3 Η HH 1.32 nd 180 ch3 H ethyl ch3 HH 1.22 nd 181 H chf2 ethyl hydrazine HH 2.00 nd 182 H chf2 ethyl ch3 HH 1.39 nd 183 H cf3 ethyl ch3 HH 1.77 nd 184 ethyl H ethyl HHH 1.59 nd 185 Ethyl H Ethyl ch3 HH 1.49 nd 186 cf3 H Ethyl ch3 HH 1.89 nd 187 HH Ethyl ch3 HH 1.11 nd 133661.doc -165 - 200917962

Ex. R41 R51 R61 Ri R2 R3 r.t. [min]; m.p. [°C] 188 chf2 H chf2 H H H 1.73 ; n.d. 189 chf2 H chf2 ch3 H H 1.66 ; n.d. 190 cf3 H chf2 H H H 2.00 ; n.d. 191 cf3 H chf2 ch3 H H 2.05 ; n.d. 192 H cf3 chf2 H H H 1.90 ; n.d. 193 H cf3 chf2 ch2-cn H H 2.43 ; n.d. 194 H chf2 chf2 H H H 1.82 ; n.d. 195 H cf3 chf2 ch3 H H 1.77 ; n.d. 196 H cf3 ch3 H H H 1.49 ; n.d.; (作為鹽酸鹽) 197 chf2 H ch3 H H H 1.46 ; n.d.; (作為鹽酸鹽) 198 cf3 H 2,2,2-三氟-乙基 H H H 1.93 ; n.d.; (作為鹽酸鹽) 199 cf3 H 4_硝基苯基 H H H 2.23 ; n.d.; (作為鹽酸鹽) 200 H H 異丙基 H H H 1.36 ; n.d.; (作為鹽酸鹽) 201 chf2 H 3-甲基-3 Η- H H H 1.11 ; n.d.; 1,3,4-三嗪-2-基 (作為鹽酸鹽) 202 H cf3 ch3 正丙基 H H 1.98 ; n.d.; (作為鹽酸鹽) 203 ch3 H 2,2,2-三氟-乙基 ch3 H H 1.43 ; n.d.; (作為鹽酸鹽) 204 H H 2,2-二氟-乙基 ch3 H H 1.10 ; n.d. 205 H H cf3 H H H n.d. ; 208 206 H chf2 乙基 ch2-cn H H 1.75 ; n.d. 207 cf3 H chf2 ch2-cn H H 2.47 ; n.d. 208 ch3 H chf2 H H H 1.50 ; n.d. 209 H ch3 chf2 H H H 1.54 ; n.d. 210 chf2 H chf2 CN H H 2.10 ; n.d. 211 cf3 H ch3 ch2-cn H H 2.02 ; n.d. 212 ch3 H ch3 ch2-cn H H 1.47 ; n.d. 213 H H chf2 H H H n.d. ; 174 214 chf2 H cf3 ch2-cn H H 2.21 ; n.d. 215 ch3 H 2,2,2-三氟-乙基 ch2-cn H H 1.76 ; n.d. 216 chf2 H ch3 ch2-cn H H 2.29 ; n.d. 217 cf3 H 乙基 ch2-cn H H 2.04 ; n.d. 218 乙基 H 乙基 ch2-cn H H 1.70 ; n.d. 219 H H 2,2,2-三氟-乙基 ch3 H H n.d. ; 90 220 ch3 H chf2 ch3 H H 1.35 ; n.d. 221 ch3 H chf2 ch2-cn H H 1.72 ; n*d. 133661.doc -166- 200917962Ex. R41 R51 R61 Ri R2 R3 rt [min]; mp [°C] 188 chf2 H chf2 HHH 1.73 ; nd 189 chf2 H chf2 ch3 HH 1.66 ; nd 190 cf3 H chf2 HHH 2.00 ; nd 191 cf3 H chf2 ch3 HH 2.05 ; nd 192 H cf3 chf2 HHH 1.90 ; nd 193 H cf3 chf2 ch2-cn HH 2.43 ; nd 194 H chf2 chf2 HHH 1.82 ; nd 195 H cf3 chf2 ch3 HH 1.77 ; nd 196 H cf3 ch3 HHH 1.49 ; nd; Acid salt) 197 chf2 H ch3 HHH 1.46 ; nd; (as hydrochloride) 198 cf3 H 2,2,2-trifluoro-ethyl HHH 1.93 ; nd; (as hydrochloride) 199 cf3 H 4 nitro Phenyl HHH 2.23; nd; (as hydrochloride) 200 HH isopropyl HHH 1.36; nd; (as hydrochloride) 201 chf2 H 3-methyl-3 Η-HHH 1.11 ; nd; 1,3,4 -triazin-2-yl (as hydrochloride) 202 H cf3 ch3 n-propyl HH 1.98; nd; (as hydrochloride) 203 ch3 H 2,2,2-trifluoro-ethyl ch3 HH 1.43 ; (as hydrochloride) 204 HH 2,2-difluoro-ethyl ch3 HH 1.10 ; nd 205 HH cf3 HHH nd ; 208 206 H chf2 ethyl ch2-cn HH 1.75 ; nd 207 cf3 H chf2 ch2-cn HH 2.47 ; nd 208 ch3 H chf2 HHH 1.50 ; nd 209 H ch3 chf2 HHH 1.54 ; nd 210 chf2 H chf2 CN HH 2.10 ; nd 211 cf3 H ch3 ch2-cn HH 2.02 ; 212 ch3 H ch3 ch2-cn HH 1.47 ; nd 213 HH chf2 HHH nd ; 174 214 chf2 H cf3 ch2-cn HH 2.21 ; nd 215 ch3 H 2,2,2-trifluoro-ethylch2-cn HH 1.76 ; nd 216 chf2 H ch3 ch2-cn HH 2.29 ; nd 217 cf3 H ethyl ch2-cn HH 2.04 ; nd 218 ethyl H ethyl ch2-cn HH 1.70 ; nd 219 HH 2,2,2-trifluoro-ethyl ch3 HH nd ; 90 220 ch3 H chf2 ch3 HH 1.35 ; nd 221 ch3 H chf2 ch2-cn HH 1.72 ; n*d. 133661.doc -166- 200917962

Ex, R41 R51 R61 ri R2 R3 r.t. [min】; m.p. [°C] 222 H H chf2 ch3 H H 1.11 ; n.d. 223 H H ch3 ch2-cn H H 1.53 ; n.d. 224 H H 乙基 ch2-cn H H 1.34 ; n.d. 225 cf3 H 4-(三氟-甲基) 苯基 H H H 2.68 ; n,d· 226 cf3 H 4-曱氧基-苯基 H H H 2.25 ; n.d. 227 cf3 H 4-(甲基-磺醯 基)-苯基 H H H 1.85 ; n.d. 228 cf3 H 4-氟苯基 H H H 2.26 ; n.d. 229 H ch3 chf2 ch3 H H 1.40 ; n.d. 230 H ch3 chf2 ch2-cn H H 1.76 ; n.d. 231 ch3 H 4-石肖基苯基 H H H 2.04 ; n.d. 232 H cf3 2,2-二氣乙基 H H H 1.81 ; n.d. 233 H H cf3 ch3 H H 1.49 ; n.d. 234 H cf3 2,2_二氟乙基 ch3 H H 1.76 ; n.d. 235 H H 2,2-二乱-乙基 ch2-cn H H 1.40 ; n.d. 236 H H 2,2,2-三氟-乙基 ch2-cn H H 1.76 ; n.d. 237 cf3 H 2,4-二氟-苯基 H H H 2.32 ; n.d. 238 cf3 H 4-曱苯基 H H H 2.50 ; n.d. 239 cf3 H 3,5-二氣-苯基 H H H 2.87 ; n.d. 240 H chf2 ch3 ch2-cn H H 1.57 ; n.d. 241 H chf2 ch3 ch3 H H 1.29 ; n.d. r.t. 保留時間 m. p. 炫點 n. d. 未測定 其他化合物242及243可根據上述方法來製備。Ex, R41 R51 R61 ri R2 R3 rt [min]; mp [°C] 222 HH chf2 ch3 HH 1.11 ; nd 223 HH ch3 ch2-cn HH 1.53 ; nd 224 HH ethyl ch2-cn HH 1.34 ; nd 225 cf3 H 4-(Trifluoro-methyl)phenyl HHH 2.68 ; n,d· 226 cf3 H 4-decyloxy-phenyl HHH 2.25 ; nd 227 cf3 H 4-(methyl-sulfonyl)-phenyl HHH 1.85 ; nd 228 cf3 H 4-fluorophenyl HHH 2.26 ; nd 229 H ch3 chf2 ch3 HH 1.40 ; nd 230 H ch3 chf2 ch2-cn HH 1.76 ; nd 231 ch3 H 4-Shischyl phenyl HHH 2.04 ; nd 232 H cf3 2,2-diqiethylHHH 1.81; nd 233 HH cf3 ch3 HH 1.49 ; nd 234 H cf3 2,2_difluoroethyl ch3 HH 1.76 ; nd 235 HH 2,2-disorder-ethyl ch2-cn OH 236 HH 2.40 ; ; nd 239 cf3 H 3,5-diqi-phenyl HHH 2.87 ; nd 240 H chf2 ch3 ch2-cn HH 1.57 ; nd 241 H chf2 ch3 ch3 HH 1.29 ; ndrt retention time mp hyun nd untested Other compounds 242 and 243 may be prepared according to the method described above.

(243): r.t. = 2.24 min h3c 2.殺蟲活性之評估: 133661.doc -167- 200917962 II.1棉蚜(棉财(aphisgossypii),混合生命期) 在50:50(體積:體積)丙酮:水及丨〇〇沖1111^1^丨以丁&quot;表面活 性劑中調配活性化合物。 藉由將受到嚴重侵擾之主群落葉片置於每一子葉頂部來 擾子葉期之棉花植株(一株植物/盆)。保持過夜以將蚜蟲 轉移至宿主植株上,且移除用於轉移蚜蟲之葉片。在測試 溶液中浸泡子葉並使其乾燥。5天後,實施死亡率計數。 在此測試中,與未經處理之對照相比,化合 \ 5、 6、 10、 11、 13、 14、 15 22 ' 23、24、25、26、28、 37、 38、 39、 40、 41 、 43 、 50、51、62 ' 65、66、67、 80、82、83、85、86、87、 95 ' 96. 97 、 98 、 99 ' 1〇〇 、 108、109、110、115、1 16、 123 、 124 、 125 、 126 、 127 、 133 、 134 、 135 、 136 、 137 、 144、 145 、 147 、 148 、 149 157 、 158 、 161 、 163 、 164 170 、 172 、 173 、 174 、 175 181 、 182 、 183 、 184 、 185 191 、 192 、 193 、 194 、 195 202 、 203 、 204 、 205 、 206 212 、 213 、 214 、 215 、 216 16 、 17 、 18 、 19 、 20 、 21 、 29 、 30 、 31 、 32 、 35 、 36 、 44、45、46、47、48、49、 69、70、71、72、73、75、 88、89、91、92、93、94、 102 、 1〇3 、 104 、 1〇5 、 1〇7 、 118 、 119 、 120 、 !21 、 122 、 128 、 129 、 130 、 131 、 132 、 138 、 139 、 141 、 142 、 143 、 150 、 151 、 154 、 155 、 156 、 165 ' 166 、 167 、 168 、 169 、 176 、 177 、 178 、 179 、 18〇 、 186 ' 187 、 188 、 189 、 190 、 196 、 197 、 199 、 200 、 201 、 207、208、209、210、21 1、 217 、 218 、 219 、 220 、 221 、 133661.doc •168- 200917962 222 、 223 、 224 、 225 、 226 、 227 、 228 、 229 、 230 、 233 、 242及243分別在300 ppm下展示至少75%之死亡率。 II.2桃蚜(煙蚜(Myzuspersicae),混合生命期) 在50:50(體積:體積)丙酮:水及1〇〇 ppm KineticaTM表面活 性劑中調配活性化合物。 藉由將受侵擾葉片部分置於測試植株頂部,用約4〇只實 驗室培養之財蟲侵擾2對葉期之胡椒植株(品種(243): rt = 2.24 min h3c 2. Evaluation of insecticidal activity: 133661.doc -167- 200917962 II.1 cotton aphid (aphisgossypii, mixed life) at 50:50 (vol: volume) acetone : Water and sputum 1111 ^ 1 ^ 丨 Ding &quot; surfactant in the preparation of active compounds. Cotton plants (one plant/pot) in the cotyledonary stage are disturbed by placing the heavily infested main community leaves on top of each cotyledon. The overnight stay was carried out to transfer the aphids to the host plants and the leaves for transfer of the aphids were removed. The cotyledons are soaked in the test solution and allowed to dry. After 5 days, mortality counts were performed. In this test, compound \ 5, 6, 10, 11, 13, 14, 15 22 ' 23, 24, 25, 26, 28, 37, 38, 39, 40, 41 compared to the untreated control , 43, 50, 51, 62 ' 65, 66, 67, 80, 82, 83, 85, 86, 87, 95 ' 96. 97 , 98 , 99 ' 1〇〇, 108, 109, 110, 115, 1 16, 123, 124, 125, 126, 127, 133, 134, 135, 136, 137, 144, 145, 147, 148, 149 157, 158, 161, 163, 164 170, 172, 173, 174, 175 181 , 182 , 183 , 184 , 185 191 , 192 , 193 , 194 , 195 202 , 203 , 204 , 205 , 206 212 , 213 , 214 , 215 , 216 16 , 17 , 18 , 19 , 20 , 21 , 29 , 30 , 31, 32, 35, 36, 44, 45, 46, 47, 48, 49, 69, 70, 71, 72, 73, 75, 88, 89, 91, 92, 93, 94, 102, 1〇3 , 104, 1〇5, 1〇7, 118, 119, 120, ! 21, 122, 128, 129, 130, 131, 132, 138, 139, 141, 142, 143, 150, 151, 154, 155, 156, 165 ' 166, 167, 168, 169, 176, 177, 178, 179 , 18 〇 , 186 ' 187 , 188 , 189 , 190 , 196 , 197 , 199 , 200 , 201 , 207 , 208 , 209 , 210 , 21 1 , 217 , 218 , 219 , 220 , 221 , 133661.doc • 168- 200917962 222, 223, 224, 225, 226, 227, 228, 229, 230, 233, 242 and 243 exhibit at least 75% mortality at 300 ppm, respectively. II.2 Myzus persica (Myzuspersicae, mixed life) The active compound is formulated in 50:50 (vol:vol) acetone:water and 1 〇〇ppm KineticaTM surfactant. By placing the infested leaf portion on top of the test plant, infesting 2 pairs of leaf stage pepper plants with about 4 实 laboratory-grown insects (variety)

Wonder’)。24小時後’移除葉片部分。在測試化合物之梯 度溶液中浸泡完整植株之葉片,並使其乾燥。在約饥及 2〇_4〇%相對濕度下將測試植株保持在螢光燈下(24小時光 、』)幻自對於校驗植株上财&amp;之死亡率測定經處 理植株上之死亡率。 在此測試中,與未經處理之對照相比’化合物丨、3 6 1〇 、 11 、 13 、 14 、 15 、 16 、 17 、 18 、 19 、 20 、 21 22、23、24、25、26、27 37、39、40、41、43、45 65、66、67、69、70、71 83、85、86、87、88、89 97、98、99、1〇〇、1〇2、 1〇9 、 110 、 115 、 116 、 118 124 、 125 、 126 、 127 、 128 134 、 135 、 136 、 137 、 138 144 、 145 、 147 、 148 、 149 157 、 158 、 161 、 ι63 、 164 、29、30、31、32、35、36、 、46 ' 47、48、49、50、62、 、73、75、79、80、81、82、 、91、92、93、94 ' 95、96、 103、1〇4、1〇5、1〇7、108、 119' 120 &gt; 121 ' 122 ' 123 &gt; 129 、 130 、 131 、 132 、 133 、 139 、 140 、 141 、 142 、 143 、 150 、 151 、 154 、 155 、 156 、 165 、 166 、 167 、 168 、 169 、 133661.doc •169- 200917962 170 、 172 、 173 、 174 、 175 、 176 、 177 、 178 、 179 、 180 、 181 ' 182 、 183 、 184 、 185 、 186 、 187 、 188 、 189 、 190 、 192 、 193 、 194 、 195 、 196 、 197 、 199 、 200 、 201 、 202 、 203 、 204 、 205 、 206 、 207 、 208 、 209 、 210 、 211 、 212 、 213 、 214 ' 215 、 216 、 217 、 218 、 219 、 220 、 221 、 222 、 223 、 224 、 225 、 226 、 227 、 228 、 229 、 233 、 242及243分 別在300 ppm下展示至少50%之死亡率。 II.3 Sr 豆財(豆財(aphis craccivora)) 在50:50(體積:體積)丙酮:水中調配活性化合物。在使用 當天製備測試溶液。 在記錄害蟲種群後對移居有丨〇〇_丨5 〇只蚜蟲之不同階段 之盆栽紅豆植株實施喷灑。在24、72、及120小時後評價 種群減少。 在此測試中,與未經處理之對照相比,化合物1、3、 5、6、7、9、10、11、13、14、15、16、17、18、19、 20、21、22、23、24、25、26、28、29、30、31、33、 35、36、38、39 ' 40、43、44、45、46、47、62、65、 66、67、69、70、72、73、75、79、80、81、82、83、 85、86、87、88、89、90、91、92、93、94、95、97、 98、99、100、1〇2、1〇3、1〇4、1〇6、107、108、1〇9、 110、 113、 114、 115' 116、 117、 118、 119、 120、 121、 122 、 123 、 124 、 132 、 133 、 134 、 135 、 136 、 138 、 139 、 141 、 142 、 143 、 144 、 145 、 147 、 148 、 149 、 156 、 157 、 158 、 161 、 163 、 164 、 165 、 166 、 167 、 168 、 169 、 17〇 、 133661.doc -170· 200917962 172 、 174 、 175 、 176 、 177 、 178 、 179 、 180 、 181 、 182 、 183 、 184 、 185 、 186 、 187 、 188 、 189 、 190 、 191 、 192 、 193 、 194 、 195 、 196 、 197 、 198 、 199 、 200 、 201 、 202 、 203 、 204 、 205 、 206 、 207 、 208 、 209 、 210 、 211 、 212 、 213 、 214 、 215 、 216 、 217 、 218 、 219 、 220 、 221 、 222 、 223、224、242及243分別在300 ppm下展示至少75%之死 亡率。 II.4豆蚜(蠶豆蚜) 在50:50(體積:體積)丙酮:水及1〇〇 ppni KineticaTM表面活 性劑中調配活性化合物。 藉由將經侵擾受切植株置於測試植株頂部用約2_3〇只實 驗室培養的财蟲侵擾生長於Metro mix中之1對葉期旱金蓮 植株(品種’Mixed Jewel,)。24小時後移除受切植株。將每 一植株浸入測試溶液中以完全覆蓋葉、莖、突出種子表面 及周圍立方體表面,並使其在通風櫥中乾燥。將經處理植 株保存於約25 t及連續螢光燈下。3天後測定蚜蟲死亡 率〇 在此測試中’與未經處理之對照相比,化合物13、14、 18、20、29、75、80、94、116、122、123、126、127、 129 135、142、143、166及168分別在1〇 ppm下展示至少 90 %之死亡率。 II·5銀葉粉風(銀葉粉虱(bemisiaargentif〇iii),成蟲) 在5〇:50(體積:體積)丙酮:水及10〇 ppm KineticaTM表面活 性劑中調配活性化合物。 133661.doc -171 - 200917962 使所選棉花植株生長至子葉期卜株植物/盆)。將子葉浸 泡至測試溶液中以—入 ’、 ^_ 凡王覆盍葉片並將其置於良好通風之區 S進仃乾燥。將每—盆經處理幼苗置於塑料杯中並引入 二私虱成蟲(約3至5日齡p使用抽吸器及連接至障 壁移液管尖端之0.6 cm無毒Tyg〇n⑧管(r_36〇3)收集昆蟲。 、、:後將δ有所收集昆蟲之尖端輕輕插入含有經處理植株 之土壤中,使昆蟲爬出尖端到達供飼喂葉片上。用可重複 使用的師網蓋(15〇微米網目之聚酯篩網PeCap,購自Tetko 公司)覆蓋杯子。在約25tA2〇_4()^相對濕度下將測試 ㈣在保藏室中保持3天,其中避免直接曝露於勞光燈(24 J、特光週期)下以防止杯内熱量聚集。將植株處理3天後評 價死亡率。 在此測試中,與未經處理之對照相比,化合物16、18、 21、26、29、35、46、48、49、5〇、62、73、75、8〇、 82、83、84、89、1〇〇、102、1〇9、133、134、163、 173 18〇、212、21 5及229分別在300 ppm下展示至 少50%之死亡率。 ΙΙ·6 褐氣風(稻褐飛風(niiaparvata iugens)) 將活性化合物調配為5〇:5〇(體積:體積)丙_ :水溶液。以 0.1 /〇 (vol/vol)之比率添加表面活性劑(Aikamuis 。 在噴灑前將稻幼苗清潔並洗滌24 h。用5 ^測試溶液噴 灑盆栽稻幼苗,風乾,將其置於籠中並移入10只成蟲。將 經處理稻植株保持在28_29。(:及50-60%之相對濕度下。在 72小時後記錄百分比死亡率。 133661.doc -172- 200917962 在此測試中,與未經處理之對照相比,化合物36、65、 176及195分別在3〇〇 ppm下展示至少50%之死亡率。 工1·7南方黏蟲(南部灰翅夜蛾(spodoptera eridania),2齡幼 蟲) 在50:50(體積:體積)丙酮:水及1〇〇 ppni KineticaTM表面活 性劑中調配活性化合物。 將一對利馬豆(Sieva lima bean)之第一真葉浸入測試溶 , 液中並使其乾燥。然後將葉置於塑料多孔拉鏈封裝包中並 加入十隻二齡幼蟲。在第4天,觀測死亡率及攝食降低。 在此測試中,與未經處理之對照相比,化合物48、%、 77 、 78 、 79 、 92 、 98 、 118 、 155 、 157 、 158 、 170 、 173 、 174 、 175 、 179 、 189 、 191 、 196 、 199 、 201 、 209 、 213 、 215、218、219 ' 220、221、223、224、228 及 233 分別在 300 ppm下展示至少5〇%之死亡率。 Π.8巢菜修尾財 ( 在1:3(體積:體積)DMS0:水中以不同經調配化合物濃度 S周配活性化合物。 將旦葉盤置於填充0 8%遠脂及2 5 〇pusTM2微量滴 定板中。用2.5 μΐ測試溶液噴麗葉盤並將⑻只成年财蟲 置於微量滴定板中,然後封閉微量滴定板並在23 ± rC及 50 土 5%之相對濕度下於螢光燈下保持6天。基於存活且繁Wonder’). After 24 hours, the blade portion was removed. The leaves of the whole plant are soaked in the gradient solution of the test compound and allowed to dry. The test plants were kept under fluorescent light (24 hours light, 』) under the hunger and 2〇_4〇% relative humidity. The mortality rate of the treated plants was determined for the mortality of the plants. . In this test, 'Compound 丨, 3 6 1〇, 11 , 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 22 , 23 , 24 , 25 , 26 compared to the untreated control , 27 37, 39, 40, 41, 43, 45 65, 66, 67, 69, 70, 71 83, 85, 86, 87, 88, 89 97, 98, 99, 1 〇〇, 1 〇 2, 1 〇9, 110, 115, 116, 118 124, 125, 126, 127, 128 134, 135, 136, 137, 138 144, 145, 147, 148, 149 157, 158, 161, ι63, 164, 29, 30 , 31, 32, 35, 36, 46 '47, 48, 49, 50, 62, 73, 75, 79, 80, 81, 82, 91, 92, 93, 94 '95, 96, 103, 1〇4,1〇5,1〇7,108, 119'120 &gt; 121 '122 '123 &gt; 129, 130, 131, 132, 133, 139, 140, 141, 142, 143, 150, 151, 154, 155, 156, 165, 166, 167, 168, 169, 133661.doc • 169- 200917962 170, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181 ' 182, 183, 184 , 185, 186, 187 , 188 , 189 , 190 , 192 , 193 , 194 , 195 , 196 , 197 , 199 , 200 , 201 , 202 , 203 , 204 , 205 , 206 , 207 , 208 , 209 , 210 , 211 , 212 , 213 , 214 '215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 233, 242 and 243 exhibited at least 50% mortality at 300 ppm, respectively. II.3 Sr Beans (aphis craccivora) The active compound is formulated in 50:50 (vol:vol) acetone:water. The test solution was prepared on the day of use. After recording the pest population, the potted red bean plants that had migrated to different stages of the mites were sprayed. Population reduction was assessed after 24, 72, and 120 hours. In this test, Compounds 1, 3, 5, 6, 7, 9, 10, 11, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22 were compared to untreated controls. , 23, 24, 25, 26, 28, 29, 30, 31, 33, 35, 36, 38, 39 '40, 43, 44, 45, 46, 47, 62, 65, 66, 67, 69, 70 , 72, 73, 75, 79, 80, 81, 82, 83, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 97, 98, 99, 100, 1〇2 , 1〇3,1〇4,1〇6,107,108,1〇9, 110, 113, 114, 115' 116, 117, 118, 119, 120, 121, 122, 123, 124, 132, 133 , 134, 135, 136, 138, 139, 141, 142, 143, 144, 145, 147, 148, 149, 156, 157, 158, 161, 163, 164, 165, 166, 167, 168, 169, 17 133, 133661.doc -170· 200917962 172 , 174 , 175 , 176 , 177 , 178 , 179 , 180 , 181 , 182 , 183 , 184 , 185 , 186 , 187 , 188 , 189 , 190 , 191 , 192 , 193 , 194, 195, 196, 197, 198, 199, 20 0, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 242 and 243 exhibited at least 75% mortality at 300 ppm, respectively. II.4 Soybean meal (Broadbean meal) The active compound is formulated in 50:50 (vol:vol) acetone:water and 1 〇〇 ppni KineticaTM surfactant. A pair of leaf stage nasturtium plants (variety 'Mixed Jewel,') grown in the Metro mix was infested with the infested plants at the top of the test plants with about 2_3 〇 of the laboratory-cultured worms. The cut plants were removed after 24 hours. Each plant was immersed in the test solution to completely cover the leaves, stems, protruding seed surface and surrounding cube surface and allowed to dry in a fume hood. The treated plants were stored under approximately 25 t and continuous fluorescent lamps. Determination of aphid mortality after 3 days 〇 In this test 'Compounds 13, 14, 18, 20, 29, 75, 80, 94, 116, 122, 123, 126, 127, 129 compared to untreated controls 135, 142, 143, 166, and 168 exhibited at least 90% mortality at 1 〇 ppm, respectively. II·5 Silver leaf powder (bemisiaargentif〇iii, adult) The active compound is formulated in 5:50 (vol:vol) acetone:water and 10〇ppm KineticaTM surfactant. 133661.doc -171 - 200917962 Growth of selected cotton plants to cotyledon stage plants/pots). The cotyledons are soaked into the test solution to immerse the leaves, and the kings cover the leaves and place them in a well ventilated area. Each potted seedling was placed in a plastic cup and introduced into two private larvae (about 3 to 5 days old p using an aspirator and a 0.6 cm non-toxic Tyg〇n8 tube connected to the tip of the barrier pipette (r_36〇3) Collecting insects.,:: Gently insert the tip of the δ collected insect into the soil containing the treated plant, so that the insect climbs out of the tip to reach the feeding leaf. Use a reusable net cover (15〇 Micro-mesh polyester screen PeCap (from Tetko) covers the cup. The test (4) is kept in the storage room for about 3 days at a relative humidity of about 25tA2〇4 (), avoiding direct exposure to the worklight (24). J, special light cycle) to prevent heat accumulation in the cup. The mortality was evaluated after treating the plants for 3 days. In this test, compounds 16, 18, 21, 26, 29, 35 were compared with the untreated control. , 46, 48, 49, 5〇, 62, 73, 75, 8〇, 82, 83, 84, 89, 1〇〇, 102, 1〇9, 133, 134, 163, 173 18〇, 212, 21 5 and 229 show at least 50% mortality at 300 ppm respectively. ΙΙ·6 brown air (niiaparvata iugens) will be active Formulated to 5 〇: 5 〇 (vol: volume) propylene _: aqueous solution. Add surfactant (Aikamuis) in a ratio of 0.1 / 〇 (vol / vol.) Wash and wash the rice seedlings for 24 h before spraying. Use 5 ^ The test solution was sprayed with potted rice seedlings, air-dried, placed in a cage and transferred to 10 adults. The treated rice plants were maintained at 28-29. (: and 50-60% relative humidity. Percent mortality was recorded after 72 hours. 133661.doc -172- 200917962 In this test, compounds 36, 65, 176, and 195 exhibited at least 50% mortality at 3 〇〇 ppm, respectively, compared to untreated controls. Mycosis (Spoodoptera eridania, 2nd instar larvae) Formulated with active compound in 50:50 (vol:vol) acetone:water and 1 〇〇ppni KineticaTM surfactant. The first true leaf of Sieva lima bean was immersed in the test solution, and allowed to dry in the liquid. The leaves were then placed in a plastic porous zipper package and ten second instar larvae were added. On day 4, mortality and food intake were observed. In this test, compared to untreated controls Compounds 48, %, 77, 78, 79, 92, 98, 118, 155, 157, 158, 170, 173, 174, 175, 179, 189, 191, 196, 199, 201, 209, 213, 215, 218 219 '220, 221, 223, 224, 228, and 233 exhibited at least 5% mortality at 300 ppm, respectively. Π.8巢菜修尾财(Weigh the active compound in 1:3 (volume: volume) DMS0: water with different compound concentration S. Place the denier disc with 0 8% far fat and 2 5 〇pusTM2 In a microtiter plate, spray the leaf disc with 2.5 μΐ test solution and place (8) adult adult insects in a microtiter plate, then close the microtiter plate and incubate at 23 ± rC and 50% relative humidity Keep under the lamp for 6 days. Based on survival and complexity

殖之财蟲§平價死亡裘。缺你raI 羊…、後目測評價蚜蟲死亡率及繁殖 力。 在此測試中’化合物3'9、&quot;、13、14、16、17、18、 133661.doc -173- 200917962 19、20、21、22、23、24、25、26、28、29、62、65、 66、67 ' 69、71、72、73、75、85 ' 87、89、91 ' 93、 94、95、96、97、98 ' 99、100 ' 102、103、104、107、 108、 109、 110、 112、 116、 117、 119、 120、 121、 122、 123 、 124 、 125 、 126 、 127 、 128 、 129 、 130 、 131 、 132 、 133 、 134 、 135 、 136 、 138 、 140 、 141 、 142 、 143 、 144 、 145 、 147 、 148 、 149 &gt; 150 、 152 、 153 、 154 、 155 、 156 、 157 、 158 、 159 、 161 、 162 、 163 、 164 、 165 、 166 、 167 、 181 、 182 、 183 、 184 、 185 、 186 、 189 、 190 、 191 、 193 、 194 、 195 、 201 、 202 、 203 、 204 、 205 、 206 、 207 、 210 、 218 、 220 、 221 、 225 、 226 、 227 、 228 、 230 、 231 、 232 、 234、242及243分別在2500 mg/L之測試溶液濃度下展示至 少80%之死亡率。 II.9棉子象鼻蟲(棉鈐象曱(Anth〇n〇mus grandis)) 在75:25(體積:體積)水:dms〇中調配化合物。 關於對棉子象鼻蟲(棉鈴象曱)之控制的評價,測試單元 係由24孔微量滴定板組成’其含有昆蟲餌料及20-30只棉 鈴象曱卵。使用定製微量喷霧器以2〇 μ1將不同濃度之經調 配化合物喷灑至昆蟲部1料上’並重複兩次。施用後,在23 ± 1°C及50 ± 5 %之相對濕度下將微量滴定板培養$天。然 後目測評價卵及幼蟲之死亡率。 在此測試中’化合物19、33、62、65、66、69、μ、 85、86、87、88、92、93、94、95、99 ' ι〇ι、、 104 、 1〇5 、 1〇6 、 1〇7 、 1〇8 、 1〇9 、 11〇 、 116 、 138 、⑷、 133661.doc -174- 200917962 145 、 147 、 148 、 149 、 150 、 151 、 153 、 154 、 155 、 156 、 157 、 159 、 160 、 161 、 162 、 166 、 167 、 171 、 185 、 186 、 188 、 189 、 190 、 191 、 192 、 193 、 194 、 206 、 207 、 220 、 221、234及243分別在2500 mg/L之測試溶液濃度下展示 100%之死亡率。在此測試中,化合物! !、13、14、16、 20、22及30分別在2500 mg/L之測試溶液濃度下展示至少 5 0%之死亡率。 II.10抵抗地中海實蠅(錐形蒼蠅(Ceratitis capitata))之活 性 在1:3(體積:體積)DMSO:水中調配活性化合物。 對於對地中海實蠅之控制的評估,測試單元係由微量滴 定板組成,其含有昆蟲餌食及50至80只錐形蒼繩印。 使用疋裝微里噴霧态以5 μ 1之量將不同濃度之經調配化 合物或混合物噴灑至昆蟲餌料上,並重複兩次。施用後, 在28± 1 C及80±5 °/。之相對濕度下將微量滴定板培養5天。 然後目測卵及幼蟲之死亡率。 在此測試中’經2500 ppm化合物7、21、62、63、77、 79、84、92、100、1〇1、126、128、147、166 ' 181、 183、184、23 1、232及234處理之卵分別展示5〇%之死亡 率〇 -175- 133661.docColony of the worms § parity death 裘. Lack of your raI sheep... and visually evaluate the mortality and fertility of locusts. In this test, 'Compound 3'9, &quot;, 13, 14, 16, 17, 18, 133661.doc -173- 200917962 19, 20, 21, 22, 23, 24, 25, 26, 28, 29, 62, 65, 66, 67 '69, 71, 72, 73, 75, 85 '87, 89, 91 '93, 94, 95, 96, 97, 98 '99, 100 ' 102, 103, 104, 107, 108, 109, 110, 112, 116, 117, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 138, 140, 141, 142, 143, 144, 145, 147, 148, 149 &gt; 150, 152, 153, 154, 155, 156, 157, 158, 159, 161, 162, 163, 164, 165, 166, 167 , 181 , 182 , 183 , 184 , 185 , 186 , 189 , 190 , 191 , 193 , 194 , 195 , 201 , 202 , 203 , 204 , 205 , 206 , 207 , 210 , 218 , 220 , 221 , 225 , 226 227, 228, 230, 231, 232, 234, 242, and 243 exhibited at least 80% mortality at a test solution concentration of 2500 mg/L, respectively. II.9 Cotton larvae (Anth〇n〇mus grandis) Compounds are formulated in 75:25 (vol:vol) water:dms. Regarding the evaluation of the control of the cotton weevil (cotton bell), the test unit consisted of a 24-well microtiter plate containing 'insect bait and 20-30 boll-like eggs. Different concentrations of the formulated compound were sprayed onto the insect part 1 at 2 〇 μ1 using a custom micro sprayer and repeated twice. After application, the microtiter plates were incubated for $day at 23 ± 1 °C and 50 ± 5% relative humidity. The mortality of eggs and larvae was then visually evaluated. In this test 'compounds 19, 33, 62, 65, 66, 69, μ, 85, 86, 87, 88, 92, 93, 94, 95, 99 ' ι〇ι, 104, 1〇5, 1 〇6, 1〇7, 1〇8, 1〇9, 11〇, 116, 138, (4), 133661.doc -174- 200917962 145, 147, 148, 149, 150, 151, 153, 154, 155, 156 , 157 , 159 , 160 , 161 , 162 , 166 , 167 , 171 , 185 , 186 , 188 , 189 , 190 , 191 , 192 , 193 , 194 , 206 , 207 , 220 , 221 , 234 and 243 respectively at 2500 mg /L test solution concentration shows 100% mortality. In this test, the compound! ! , 13, 14, 16, 20, 22, and 30 exhibited at least 50% mortality at a test solution concentration of 2500 mg/L, respectively. II.10 Activity against Mediterranean fruit fly (Ceratitis capitata) The active compound was formulated in 1:3 (vol: volume) DMSO: water. For the evaluation of the control of the fruit fly, the test unit consists of a microtiter plate containing insect bait and 50 to 80 cone-shaped stalks. Different concentrations of the formulated compound or mixture were sprayed onto the insect bait in an amount of 5 μl using an armored microinjection spray and repeated twice. After application, at 28 ± 1 C and 80 ± 5 ° /. The microtiter plates were incubated for 5 days at relative humidity. The eggs and larvae were then visually observed for mortality. In this test 'via 2,500 ppm of compounds 7, 21, 62, 63, 77, 79, 84, 92, 100, 1, 1, 1, 128, 147, 166 ' 181, 183, 184, 23 1, 232 and 234 treated eggs showed 5% mortality, 〇-175- 133661.doc

Claims (1)

200917962 十、申請專利範圍·· 1. -種控制無脊椎害蟲之方法,該方法包含用殺蟲有效量 之式I或II吡唑化合物或其鹽或沐氧化物處理該等害蟲、 其食物供應、其棲息地或其繁殖地、或其中生長或可生 長該等害蟲之植物、種子、土壤、區域'材料或環境、 或欲防止受到害蟲侵襲或侵擾之該等材料、植物、種 子、土壤、表面或空間:200917962 X. Patent application scope · 1. A method for controlling invertebrate pests, which comprises treating the pests with an insecticidally effective amount of a pyrazole compound of the formula I or II or a salt thereof or a muoxide thereof, and the food supply thereof , their habitat or their breeding grounds, or plants, seeds, soils, areas that are grown or can grow such pests, materials or environments, or materials, plants, seeds, soils that are intended to be protected from pest infestation or infestation, Surface or space: A 係式Al、A2或A3之u比σ坐某A system of Al, A2 or A3 is more than σ R41R41 A2 A3 表示與式I或11之其餘部分之結合位點; X1 係 s、0 或 NRla ; X2 係 〇R2a、NR2bR2c、s(〇)mR2d; X3係孤電子對或氧; R 係氫、CN、CVCw燒基、Ci_Cl()__ 代烷基、c3_Ci〇 %烷基、C3-C10-鹵代環烷基、。{⑴環烷基甲 I3366l.doc 200917962 c3-c10-ii代環烷基甲基、c2_Cl0_烯基、c2_Cl0_鹵代 烯基、C2-C10-炔基、c3-C10-鹵代炔基、CVC4-伸烷 基-CN、〇Ra、Cl_c4-伸烷基-ORa、C(Y)Rb、CVC4-伸烧基-C(Y)Rb、C(Y)ORc、C〗-C4-伸烷基-C(Y)ORc、S(〇)2Rd、NReRf、q-CV伸烷基-NReRf、 C(Y)NRgRh 、 Ci-C4-伸烷基-C(Y)NRgRh 、 S(0)mNReRf、C(Y)NRiNReRf、苯基、雜芳基、苯基_ c〗-C4-烧基及雜芳基_Ci_c4-烷基,其中上述最後四 個基團之芳香族環可未經取代或可具有1、2、3、4 或5個相同或不同取代基Rx ; R2係氫、鹵素、CVCV烷基、CVC4-鹵代烷基、(VCV 烷氧基、CVCU-鹵代烷氧基、CVC4-烷硫基、CVC4-鹵代烷硫基、Cf-Cr烷基亞磺醯基、Cl_C4_鹵代烷基 亞磺醯基、Ci-C4-烷基磺醯基、Cl_c4_鹵代烷基磺醯 基、C3-C6-環炫^基、c3-C6-ii代環烧基、c2-C4-烯 基、C2-C4-鹵代烯基、C2-C4-炔基或烷氧基-CVC4-烷基; R3係氫、鹵素、CrCV烷基、CVCV鹵代烷基、CVC4-烷氧基、C〗-C4-鹵代烷氧基、Ci-C4-烷硫基、CVC4-鹵代烧硫基、G-C4-烧基亞石黃醯基、Cj-Cf鹵代烧基 亞磺醯基、Ci-C:4-烷基磺醯基、CrCr鹵代烷基磺醯 基、C3-C6-環烧基、C3-C6-鹵代環烷基、c2-C4-烯 基、C2-C4-鹵代烯基、C2-C4-炔基或Ci_c4_烷氧基_ CVC4-烷基; 133661.doc 200917962 m 係0、1或2 ; R41、R42、R43係選自由以下組成之群:氫、卤素、CN、 N〇2、Ci-C10-烧基、c3-C10-環烧基、C5-C10_ 環稀 基、C3-C10-環烧基曱基、c2-C10-烯基、c2-c10-块 基,其中上述最後6個基團之脂肪族或環狀部分可未 經取代、可經部分或完全!I化或可具有1、2或3個相 同或不同取代基Ry、〇Ra、SRa、C(Y)Rb、 C(Y)ORe、S(0)2Rd、NReRf、C(Y)NRgRh、苯基、苯 基-CVC4-烧基、苯氧s_Cl_c4_烧基、5員雜芳基及 雜環-CrC4-烷基,其中上述最後5個基團之雜環基 及芳香知環可未經取代或可具有1、2、3、4或5個相 同或不同取代基Rx ; 、鹵素、CN、N02、C,-c5-c1G-環烯基、C3_Ci()_ R51係選自由以下組成之群:氫、 C10-烧基、C3-C1Q-環烧基、c 環烷基甲基、C2_c10_烯基、C2_Ci〇_炔基,其中上述 最後6個基團之脂肪族或環狀部分可未經取代、可經 部分或完全鹵化或可具有!、 、2或3個相同或不同取代A2 A3 represents a binding site to the rest of formula I or 11; X1 is s, 0 or NRla; X2 is 〇R2a, NR2bR2c, s(〇)mR2d; X3 is a lone pair or oxygen; R is hydrogen, CN , CVCw alkyl, Ci_Cl () _ alkyl, c3_Ci 〇 % alkyl, C3-C10-halocycloalkyl,. {(1)cycloalkylmethyl I3366l.doc 200917962 c3-c10-ii cycloalkylmethyl, c2_Cl0-alkenyl, c2_Cl0_haloalkenyl, C2-C10-alkynyl, c3-C10-haloalkynyl, CVC4-alkylene-CN, 〇Ra, Cl_c4-alkyl-ORa, C(Y)Rb, CVC4-alkylene-C(Y)Rb, C(Y)ORc, C--C4-desane -C(Y)ORc, S(〇)2Rd, NReRf, q-CV alkylene-NReRf, C(Y)NRgRh, Ci-C4-alkylene-C(Y)NRgRh, S(0)mNReRf , C(Y)NRiNReRf, phenyl, heteroaryl, phenyl-c--C4-alkyl and heteroaryl_Ci_c4-alkyl, wherein the aromatic ring of the last four groups described above may be unsubstituted or May have 1, 2, 3, 4 or 5 identical or different substituents Rx; R2 is hydrogen, halogen, CVCV alkyl, CVC4-haloalkyl, (VCV alkoxy, CVCU-haloalkoxy, CVC4-alkyl sulfide , CVC 4-haloalkylthio, Cf-Cr alkylsulfinyl, Cl_C4_haloalkylsulfinylene, Ci-C4-alkylsulfonyl, Cl_c4_haloalkylsulfonyl, C3-C6-ring Homo-based, c3-C6-ii-substituted cycloalkyl, c2-C4-alkenyl, C2-C4-haloalkenyl, C2-C4-alkynyl or alkoxy-CVC4-alkyl; R3 hydrogen, Halogen, CrCV alkyl, CVCV haloalkyl CVC4-alkoxy, C--C4-haloalkoxy, Ci-C4-alkylthio, CVC4-halosulfonyl, G-C4-alkyl sulfite, Cj-Cf halosulfinyl Sulfhydryl, Ci-C: 4-alkylsulfonyl, CrCr haloalkylsulfonyl, C3-C6-cycloalkyl, C3-C6-halocycloalkyl, c2-C4-alkenyl, C2-C4 -haloalkenyl, C2-C4-alkynyl or Ci_c4_alkoxy_CVC4-alkyl; 133661.doc 200917962 m is 0, 1 or 2; R41, R42, R43 are selected from the group consisting of hydrogen , halogen, CN, N〇2, Ci-C10-alkyl, c3-C10-cycloalkyl, C5-C10_ ring, C3-C10-cycloalkyl, c2-C10-alkenyl, c2- C10-block group, wherein the aliphatic or cyclic moiety of the last six groups described above may be unsubstituted, may be partially or completely converted or may have 1, 2 or 3 identical or different substituents Ry, 〇Ra , SRa, C(Y)Rb, C(Y)ORe, S(0)2Rd, NReRf, C(Y)NRgRh, phenyl, phenyl-CVC4-alkyl, phenoxy s_Cl_c4_alkyl, 5-member An aryl group and a heterocyclic-CrC4-alkyl group, wherein the heterocyclic group and the aromatic ring of the last five groups described above may be unsubstituted or may have 1, 2, 3, 4 or 5 identical or different substitutions. Rx;, halogen, CN, N02, C, -c5-c1G-cycloalkenyl, C3_Ci()_R51 are selected from the group consisting of hydrogen, C10-alkyl, C3-C1Q-cycloalkyl, c-ring Alkylmethyl, C2_c10-alkenyl, C2_Ci〇-alkynyl, wherein the aliphatic or cyclic moiety of the last six of the above groups may be unsubstituted, partially or fully halogenated or may have! , , 2 or 3 identical or different substitutions 4或5個相同或不同取代基rx ; 、RM係選自由以4 or 5 identical or different substituents rx; no2、CVC】。-烷基、 C3-C10-環烧基、 C5-C1G-環浠 133661.doc 200917962 基、C3-CIG-環炫基 f 基、C2-C1()-稀基、c2-c10-块 基’其中上述最後ό個基團之脂肪族或環狀部分可未 經取代、可經部分或完全鹵化或可具有2或3個相 同或不同取代基Ry、ORa、SRa、c(Y)Rl)、 C(Y)ORc、S(0)2Rd、NReRf、C(Y)NRgRh、雜環基、 苯基、苯基-C,-C4_烷基、苯氧基-Ci_C4_烷基及雜環_ G-C:4-烷基,其中上述最後5個基團之雜環基及芳香 族環可未經取代或可具有〗、2、3、4或5個相同或不 同取代基Rx ; R61、R63係選自由以下組成之群:氫、N〇2、Ci_Ci❶-院 基、c3-c1g-環烷基、C5_Cig_環烯基、c3_Cig_環烷基 甲基、C2-Cl0_稀基、c2_Ci〇_快基,其甲上述最後6 個,團之脂肪族或環狀部分可未經取代、可經部分 或广全商化或可具有J、2或3個相同或不同取代基 NReRf〇Ra、SRa、c(Y)Rb、C⑺㈣、s(0)2Rd、 =、c〇〇NRgRh、s(())mNReRf、c⑺嶋心、 美:二笨基、笨基'Cl々烷基、苯氧基々c-烷 ί美及:r_Cl_C4·烷基,其中上述最後5個基團之雜 香族環可未經取代或可具有卜2、 5 J及不同取代基Rx ; R6‘係選自由以下組成之群… 袠燒基、C5 C :、N〇2、Cl_^ 基、C χ 5 10 %烯基、C3-C丨ο-環烷基甲 基團之r肪:基、C”C1°_炔基’其中上述最後6個 月曰肪知或環狀部分可未經取代、可經部分或 133661.doc 200917962 完全鹵化或可具有1、2或3個相同或不同取代基Ry、 ORa、SRa、C(Y)Rb、C(Y)ORc、S(0)2Rd、NReRf、 C(Y)NRgRh、s(0)mNReRf、C(Y)NRiNReRf、苯基、 苯基-Ci-CV烷基、苯氧基-c]_c4_烷基、5員雜芳基 及雜環-CrC4-烷基,其中上述最後5個基團之雜環 基及芳香族環可未經取代或可具有1、2、3、4或5個 相同或不同取代基rx ; Y 係Ο或S ; Rla係選自氫、q-Cw烷基、CVCVii代烷基、c3-C1()-環烧基、C3_C10-環烷基甲基、C3_C10-鹵代環烷基、 c2-c10-烯基、c2_Cl〇_鹵代烯基、c2_Cl〇-炔基、 c10-烧氧基-CrCV烷基、〇Ra、苯基、雜芳基、笨 基-Ci-C:4-烷基及雜芳基_Cl_C4_烷基,其中上述最後 4個基團之芳香族環可未經取代或可具有1、2、 j、4 或5個彼此獨立地選自由以下組成之群之取代基:鹵 素、氰基、硝基、Cl-C4-烷基、Cl_c4_鹵代烷基、 C1-C4-烷氧基及Cl_c4_鹵代烷氧基; R2a係選自cvcv烷基、Cl_c4_鹵代烷基、c3_C6_環烷 基、C3-C6-#代環烷基、烯基、C2_C4_自代烯 基' c2-c4-炔基、Cl-C4_烷氧基_Ci_c4_烧基、苯基、 雜芳基、苯基-Cl-C4-烷基及雜芳基烷基其 中上述最後4個基團之芳香族環可未經取代或可具有 1、2 ' 3、4或5個彼此獨立地選自由以下組成之群之 取代基:i素、氰基、硝基、Cl_c4_烷基、Ci_c^ 133661.doc 200917962 代炫基Cl-C4_炫氧基及Cl_C4-自代烧氧基; R2、R、彼此獨立地選自氫、Ci々烷基、c】々函代 烷基、c3-c6-環貌基、c3_C6峭代環烷基、c2心-烤 基、c2-c4-虐代稀基、c2_C4_块基、Ci_C4_院氧基· CVCV燒基、Cl_C4_炫基㈣、Ci_CH代燒基幾 基、CyC4·烷基磺醯基、Ci_C4__代烷基磺醯基、苯 基 '本基碳基、苯基續醯基、雜芳基、雜芳基幾 基、雜芳基石黃酿基、苯基々CV炫基及雜芳基々 C4烷基,其中上述最後8個基團中之芳香族環可未 I取代或可具有1 ' 2、3、4或5個彼此獨立地選自由 以下組成之群之取代基:画素、氰基、硝基' c丨_ c4-烧基、Cl_C4^代烷基、Ci_C4_烧氧基及^々齒 代烷氧基;或No2, CVC]. -alkyl, C3-C10-cycloalkyl, C5-C1G-cyclopropene 133661.doc 200917962, C3-CIG-cyclodextyl f, C2-C1()-saturated, c2-c10-blockyl' Wherein the aliphatic or cyclic moiety of the last one of the above groups may be unsubstituted, partially or fully halogenated or may have 2 or 3 identical or different substituents Ry, ORa, SRa, c(Y)Rl), C(Y)ORc, S(0)2Rd, NReRf, C(Y)NRgRh, heterocyclic group, phenyl group, phenyl-C, -C4_alkyl group, phenoxy-Ci_C4_alkyl group and heterocyclic ring_ GC: 4-alkyl, wherein the heterocyclic group and the aromatic ring of the last five groups described above may be unsubstituted or may have 2, 3, 4 or 5 identical or different substituents Rx; R61, R63 The following components are selected: hydrogen, N〇2, Ci_Ci❶-hospital, c3-c1g-cycloalkyl, C5_Cig_cycloalkenyl, c3_Cig_cycloalkylmethyl, C2-Cl0_thinyl, c2_Ci〇_ Fast group, the last six of which are the above, the aliphatic or cyclic moiety of the group may be unsubstituted, partially or fully commercialized or may have J, 2 or 3 identical or different substituents NReRf〇Ra, SRa , c(Y)Rb, C(7)(4), s(0)2Rd, =, c〇〇NRgRh, s(())mNReRf, c(7) </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> <RTIgt; 2, 5 J and different substituents Rx; R6' is selected from the group consisting of: anthracenyl, C5 C:, N〇2, Cl_^, C χ 5 10 % alkenyl, C3-C丨ο- a cycloalkyl group of a cycloalkyl group: a C, C1 °  alkynyl group wherein the last 6 months of the above-mentioned or acyclic moiety may be unsubstituted, may be partially or 133661.doc 200917962 fully halogenated or Having 1, 2 or 3 identical or different substituents Ry, ORa, SRa, C(Y)Rb, C(Y)ORc, S(0)2Rd, NReRf, C(Y)NRgRh, s(0)mNReRf, C(Y)NRiNReRf, phenyl, phenyl-Ci-CV alkyl, phenoxy-c]-c4-alkyl, 5-membered heteroaryl and heterocyclic-CrC4-alkyl, wherein the last five groups described above The heterocyclic group and the aromatic ring may be unsubstituted or may have 1, 2, 3, 4 or 5 identical or different substituents rx; Y system or S; Rla is selected from hydrogen, q-Cw alkyl, CVCVii alkyl, c3-C1()-cycloalkyl, C3_C10-cycloalkylmethyl, C3_C10-halocycloalkyl, c2-c10-ene , c2_Cl〇_haloalkenyl, c2_Cl〇-alkynyl, c10-alkoxy-CrCV alkyl, 〇Ra, phenyl, heteroaryl, phenyl-Ci-C: 4-alkyl and heteroaryl _Cl_C4_alkyl, wherein the aromatic ring of the last four groups described above may be unsubstituted or may have 1, 2, j, 4 or 5 substituents independently of each other selected from the group consisting of halogen, cyanide a base, a nitro group, a Cl-C4-alkyl group, a Cl_c4_haloalkyl group, a C1-C4-alkoxy group, and a Cl_c4_haloalkoxy group; the R2a group is selected from the group consisting of cvcv alkyl group, Cl_c4_haloalkyl group, c3_C6_cycloalkyl group, C3-C6-# cycloalkyl, alkenyl, C2_C4_self-alkenyl' c2-c4-alkynyl, Cl-C4_alkoxy_Ci_c4_alkyl, phenyl, heteroaryl, phenyl- Cl-C4-alkyl and heteroarylalkyl wherein the aromatic ring of the last four groups described above may be unsubstituted or may have 1, 2 '3, 4 or 5 independently of each other selected from the group consisting of Substituents: i, cyano, nitro, Cl_c4_alkyl, Ci_c^ 133661.doc 200917962 thiol Cl-C4_ methoxy and Cl_C4-self alkoxy; R2, R, independently of each other From hydrogen, Ci 々 alkyl, c 々 々 alkyl, c3-c6- ring c3_C6 choline cycloalkyl, c2 heart-bake base, c2-c4- abused base, c2_C4_ block, Ci_C4_homoyloxy; CVCV alkyl, Cl_C4_croplex (tetra), Ci_CH alkyl group, CyC4·alkylsulfonyl, Ci_C4__alkylsulfonyl, phenyl 'benyl carbon, phenyl fluorenyl, heteroaryl, heteroaryl, heteroaryl, phenyl And a heteroaryl 々C4 alkyl group, wherein the aromatic ring in the last 8 groups may be unsubstituted or may have 1 '2, 3, 4 or 5 independently of each other selected from the group consisting of Substituents of the group: a pixel, a cyano group, a nitro 'c丨_c4-alkyl group, a Cl_C4 alkyl group, a Ci_C4_ alkoxy group, and a dentate alkoxy group; mie與其所鍵結之氮原子_起形成5•或6員飽和或不 飽和雜環’其可具有選自〇、之另一雜原子作 為環成員原子且其中該雜環可未經取代或可具有i、 2、3、4或5個彼此獨立地選自由以下組成之群之取 代基:函素、氰基、硝基、Cl_C4{基、^代 烷基、CVCV烷氧基及CVC^鹵代烷氧基; R係選自(VC4-烧基、q-cv _代烷基、c3_C6_環烧 基、C3-C6-鹵代環炫基、c2_c4_稀基、C2_C4_ _代稀 基、C2-C4-炔基、CVC4-烧氧基_Ci_c4_烧基、苯基、 雜方基、苯基-CrC4-烷基及雜芳基·Ci_c4_烷基,其 中上述最後4個基團之芳香族環可未經取代或可具有 133661.doc 200917962 R8 R( Re 1、2、3、4或5個彼此獨立地選自由以下組成之 :代基:函素、氰基、確基、Ci々烧基、c〜 燒基、Cl_C4_燒氧基及Ci_C4-南代烧氧基; 〜係彼此獨立地選自氫、Ci々烧基、Ci_c^ 代燒基、C3_C6_環燒基、c3-c6·環院基甲基、C”C6 自代環烧基、q-CV晞基、C2_C4•函代烯基、c2_c :基、Cl-C4-烧氧基_Cl々烧基、苯基、雜芳基: 本基-C丨-(V烧基及雜芳基基,其中上述 後4個基團之芳香族環可未經取代或可具有i、2、 3、4或5個彼此獨立地選自由以下組成之群之取代 基:齒素、氰基、硝基、Ci々烷基、Ci々齒代院 基、CVC4·烷氧基及Ci_C4_鹵代烷氧基; 係選自CVC4-烷基、C1々幽代烷基、C3_C6_環烷 基' c3-c6-環烷基甲基、C3_C6确代環烷基、 稀基、c2_c4_南代烯基、C2_C4_炔基、Ci_c4_院氧基_ ycv烧基、笨基、雜芳基、苯基夂'_烧基及雜 方基-Cl-C4_烷基,其中上述最後4個基團之芳香族 環可未經取代或可具有1、2、3、4或5個彼此獨立地 選自由以下組成之群之取代基:_素、氛基、硝 基、cvk院基、Ci_C4_鹵代烧基、ΙΑ道氧基及 Ci-C4-鹵代烧氧基; ,彼此獨立地選自氫、Ci_C4_烧基、Ci_c4^代烧 f、C3-C6-環院基、C3_C6•環烷基曱基、C3_C6_函代 環烷基、C2-(V烯基、C2_C4_由代烯基、c2心-块 133661.doc 200917962 基、kcv貌氧基_Cl_C4道基、Ci_c4_燒基幾基、 Cl-CV齒代烷基羰基、c^c4-烷基磺醯基、Ci_C4-齒 ,烧基續酿基、苯基、笨基幾基'苯基績醯基、雜 芳土雜芳基羰基、雜芳基磺醯基、苯基_C|_C4_烷 基,雜方基-CrCV烧基’其_上述最後8個基圓中 之芳香族環可未經取代或可具有J、2、3、4或5個彼 此獨立地選自由以下組成之群之取代基:齒素、氰 基、硝基、CVCV烧基、Cl_c4_画代炫基、Ci_c4炫 氧基及Ci-Cr鹵代烷氧基;或 R及R與其所鍵結之氮原子形成5_或6員飽和或不飽 t雜環,其可具有選自〇、s&amp;N之另—雜原子作為 環成員原子且其中該雜環可未經取代或可具有i、 2、3、4或5個彼此獨立地選自由以下組成之群之取 代基:鹵素、氰基、硝基、Cl_c4_烧基、Ci_c一代 烷基、CrC4·烷氧基及(^-(:4-鹵代烷氧基; Rg、Rh係彼此獨立地選自氫、Cl_c4_烷基、Ci_c4__代烷 基、c3-c6-環烧基、C3-C6-i代環烧基、c2_c44 基、C2-C4-鹵代稀基、C2-C4-块基、Cl_c4•院氧基_ Cl-C4-烷基、苯基、雜芳基、苯基-(:1&lt;4_烷基及雜 芳基-C^-C4·烷基,其中上述最後4個基團之芳香族 %可未經取代或可具有1、2、3、4或5個彼此獨立地 選自由以下組成之群之取代基:_素、氰基、硝 基、CVC4-炫基、(VC4-鹵代烷基、Cl-c4-烷氧基及 C1-C4-鹵代炫氧基; 133661.doc 200917962 R,係選自由以下組成之群:A、Cl-c4-烧基、Cl-C4齒 代烷基、c3-c6-環;1¾基、c3_c6環烧基甲基、C3_C6_ 白代%燒基、C2-C4-缔基、c2_c4_ _代烯基、C2_C4_ 炔基、Cl-C4_烷氧基-C丨-cv烷基、苯基及苯基_Cl_ 4烷基,其中上述最後2個基團中之苯環可未經取 代或可具有1、2 ' 3、4或5個彼此獨立地選自由以下 、、且成之群之取代基:鹵素、氰基、硝基、Ci_c4_烷 基、c^-c:4-鹵代烧基、Cl_C4_烷氧基及Ci_C4_鹵代烷 氣基; Rx係選自由以下組成之群:鹵素、氰基、硝基、Cl_ C4-烷基、(VC4-鹵代烷基、CVC4-烷氧基、CVC4-鹵 代烷氧基、(VC4-烷硫基、CVC4-鹵代烷硫基、C,-C4-烧基亞石頁酿基、Ci-C4_鹵代院基亞石黃酿基、C 1 -c4-烷基磺醯基、Ci-Cr鹵代烷基磺醯基、c,-c4-烷 基羰基、CVC4-鹵代烷基羰基、c3-c6-環烷基、c3-c6-鹵代環烷基、c2-c4-烯基、c2-c4-鹵代烯基、c2-c4-炔基及CVC4-烷氧基-CrCU-烷基; Ry係彼此獨立地選自C1-C4-烧基、C1-C4-鹵代烧基、 C1-C4-烧氧基、C1-C4-鹵代院氧基、C1-C4-烧硫基、 C1-C4-鹵代烧硫基、ci-c4-烧基亞石夤酸基、Ci_C4_鹵 代烧基亞績醯基、C1-C4_烧基確醯基、Cl_C4_鹵代烧 基磺醯基、C3-C6-環烷基、CVCe-鹵代環烷基、C2· C4-烯基、C2-C4-鹵代烯基、C2-C4-炔基、G-C4-烧氧 基-CVC4-烷基及CVCn-烷基羰基。 133661.doc -9- 200917962 2. 如睛求項1之方法,其中該吡唑化合物係式j化合物。 3. 如請求項1之方法,其中該吡唑化合物係式〗化合物,其 中式I中之X1為氧。 4. 如晴求項1之方法,其甲該吡唑化合物係式丨化合物,其 中Rl係氫、CN、Cl-Cl0-烷基、Cl-Cl〇_鹵代烷基、c2· Cio-烯基、c2-C10-鹵代烯基、C2-C10-炔基、C^-CV烷氧 基-Cl~cio-烧基、CVC4-伸烷基-CN、〇Ra、C(Y)Rb、 c(Y)〇Re或 s(o)2Rd。 5. 如請求項4之方法,其中R丨係氫、CrCV烷基或Cl_c4_伸 炫基-CKf。 6.如π求項!之方法,其中R2係氫、曱基、二氟甲基、三 氟甲基、甲氧基、二氟甲氧基或三氟曱氧基。 7·:請求項!之方法,其中r3係氫、甲基、二氟甲基、三 氣:基甲氧基、二氟甲氧基或三氟曱氧基=&gt; 8.如μ求項6或7之方法,其中該等基團 係氫。 4 夕1固 9 ·如請求項8 $ t &amp; 、方法,其中基團R2及R3二者皆為氫。 1〇_如凊求項丨至7中 η.如請求項ίο之方* Γ 係基團A1。 素、CN、 法、中R4丨及R51係獨立地選自氫、齒 ’、 、Cl-C1G-垸基、C, Γ « 广 C2-C丨0-炔美,甘屮 1〇-衣烷基、C2-C丨〇烯基及 N 八 上述最後4個基團中之脂肪族1 部分可未經敗冲π Α Τ夂钿妨禊或%狀 η °邛分或完全鹵化或可具有}咬2個 同或不同取代基Ry。 A 2個相 12 ·如請求項丨 ',其中R41及R51係彼此獨立地選自 133661.doc -10- 200917962 風、CN、鹵素、C丨-c4-烷基、C丨-c4- _代烷基、c3_c 裱烷基及C3_C6· _代環烷基。 13. 如請求項12之方法,其中R41及R51係彼此獨立地選自 氫、CN、鹵素、CH3、CH2f、CHf2及 cf3。 14. 如請求項13之方法,其中R41或R51為氫或R41及R51二者皆 15·如請求項10之方法,其中R61係選自由以下組成之群: Cl ClG_燒基、代炫•基、C3-C1G-環烧基、c3_c10_ 鹵代%烷基、C3_C10-環烷基甲基、C3-C10-鹵代環烷基甲 基、c2-c10-烯基、c2-C10-齒代烯基、CrCr烷氧基_Ci_ c1〇-烷基、苯基、苄基、苯氧基_〒基、5_或6員雜芳 基、5-或6員雜芳基甲基,其中上述最後5個基團中之 (雜)芳香族環可未經取代或可具有丨、2、3、4或5個相同 或不同取代基RX,其係選自鹵素、Ci_C4_烷基、 代烷基、Ci-CV烷氧基、C丨-(V鹵代烷氧基、c丨·c4_烷基 確醯基、及Ci-CU-鹵代烷基磺醯基。 16_如請求項15之方法,其中R6,係C〗_C4_烷基或C1_C4__代 烷基。 17. 如請求項丨至7中任一項之方法,其中A為基團A2。 18. 如請求項17之方法,其中R42係選自氫、鹵素、 c4-院基、Cl-c4嗰代院基、C3_C]G_環烧基、匕_^__代 環烷基及苯基,其可未經取代或可具有丨、2、3、4或5 個相同或不同取代基V,其係選自ώ素、Ci_C4烷基、 CVCV鹵代烷基、CVCV烷氧基及^/广鹵代烷氧基。 133661.doc -11 - 200917962 19.如請求jg彳s 4 &amp; 、8之方法,其中R42係選自氫、卣素、CN 匕4·院基、Γ 上, 匕1- i-C4-鹵代烷基、C3-C6-環烷基及c c 環烷基。 &quot;·叹鹵代 20·如請求jg〗7 + + 氫、自♦ 法,其中R52係選自由以下組成之群: ”、CN、c】-cI0-坑基、Cl_Cl“ 代 c c ^ C3_Cl〇-鹵代環烷基、c3-c10-環烷基甲基、 3 代環烷基曱基、C2-CI()-烯基、 ^基-c]-c丨0-燒基、苯基、节基、苯氧A_ T -¾ ' AL· λ*- ** 土 貝雜方基、5-或6員雜芳基甲基,其中上、十、 2取個基團中之(雜)芳香族環可未經取代或可且有1 貌基4或:個:同^ C1-C4-幽代烷基、Ci_c4_烷 烷氧基、h-c4-鹵代 1 c4-烷基嶒醯基、及Ci_ 21. 如請求項加夕士 口代沉基%醯基。 氮、1Γ ’其中R52係選自由以下組成之群: 致幽素、™、Cl_Cl。-烧基、CH齒代烧 Cio-環烷基、c Γ 占 k 土(:3- C-C ^ 鹵代環烧基、4-(^-環院基甲基、 3 10 ·'代%烷基甲基、c2-cI0-烯基、c c 及Ci-C4-;Jt氧A p ^ 2-C1(r卣代烯基 疋乳基-Ci_C丨0-烷基。 22. 如請求 尺項17之方法,其中r62係選 氫、kc10道基、CVC南代广其下組成之群: C3-C 1 Cl0-鹵代烷基、C3-Cl0-環烷基、 c“i〇·自代環院基、c”Ci0•環院基甲 烷基甲基、C,C、法1 c3-c丨0-_代環 基-CVC ^ Cl^代歸基、Cl-C4_烧氧 土 1丨c丨〇-烷基、苯基 基,兑中上、…么 貝雜方基、节基及苯氧基曱 返最後4個基團之芳香族環可未經取代或可 133661.doc -12- 200917962 具有1、2、3、4或5個相同或不同取代基RX,其係選自 鹵素、CVCV烷基、(Vc4-鹵代烷基、cvcv烷氧基、 C1-C4-鹵代炫乳基、G-C4-燒基石黃醯基、及Q-C4-鹵代p 基績酿基。 23. 如請求項22之方法’其中R62係氫、c丨-C4-烷基或 鹵代炫基。 24. 如請求項1至7中任一項之方法,其中a為基團A3。 25. 如請求項24之方法’其中R43係選自氫、鹵素、CN、r c4_烧基、C丨-C4-鹵代烷基、c3_Cl〇_環烷基、c3_Ci〇_南代 環烷基及苯基,其可未經取代或可具有1 ' 2、3、4或5 個相同或不同取代基Rx,其係選自鹵素、Ci_C4_烷基、 CVC4-鹵代烷基、CVC4-烷氧基、Cl_C4_鹵代烷氧基、 C1-C4·烷基磺醯基、及Ci-C*-鹵代烷基磺醯基。 26. 如請求項2S之方法,其中r43係選自氫、鹵素、CN、 c4-烷基、CVC4-鹵代烷基、c3_c6_環烷基及c3_c6•鹵代 環烷基。 27. 如請求項24之方法,其中R53係選自由以下組成之蛘. 氫、鹵素、CN、(:,-(:〗〇-烷基、(:,-(:〗〇-鹵代烷基' c3_ Ci〇-環烷基' C3-C10-鹵代環烷基、c3_C10-環烷基曱基、 c3-c丨0-鹵代環烷基曱基、C2_Ci〇•烯基、C2_Ci〇_ _代烯 基、Ci-cv燒氧基_Cl—Cl(r烷基、笨基、苄基、苯氧基_ 曱基、5-或6員雜芳基、5_或6員雜芳基甲基,其中上述 最後5個基團中之(雜)芳香族環可未經取代或可具有i、 2、3、4或5個相同或不同取代基RX,其係選自鹵素、 133661.doc -13· 200917962 c4-烧基、CVC4-鹵代炫基、Cl_C4_烧氧基' c〗_c4-鹵代 烷氧基、CVC4-烷基磺醢基、及Cl_C4_函代烧基績酿基。 28.如請求項27之方法,其中r53係選自由以下組成之群: 氫、鹵素、CN、Ci-Cio-烧基、Ci-C10_鹵代烧基、匸3_ Ci〇 -環院基、C3_Ci〇-鹵代環烧基、C3_Ci〇-i衣烧基甲基、 C3-C10-鹵代環烧基曱基、C2-C10-稀基、C2-C10-鹵代稀基 或C 1 - C 4 -院氧基_ C 1 - C 1 0 -烧基。 29.如請求項24之方法,其中R63係選自由以下組成之群: 鼠、Ci-Ci〇-烧基、Ci-Ci〇-鹵代院基、C3-C10-環燒基、 C3-C10-鹵代環烧基、C3-C10 -環烧基甲基、C3-C10-鹵代環 烧基曱基、C2-Ci〇-稀基、C2-C10-鹵代稀基、Ci-C4-;^氧 基-CrC^o-烷基、苯基、苄基、苯氧基-曱基、5_或6員雜 芳基、5-或6員雜芳基甲基,其中上述最後5個基團中之 (雜)芳香族環可未經取代或可具有1、2、3、4或5個相同 或不同取代基Rx ’其係選自鹵素、Cl_C4_烷基、Ci_C4-函 代烧基、CVC4-院氧基、Ci-C4-鹵代院氧基、燒基 確酸基、及Ci-C4-鹵代烷基磺醯基。 30.如請求項29之方法,其中r53或R63係氫、Ci_C4_烷基或 G-C:4-鹵代烷基,同時R53、R63之另一基團係選自由以下 、、且成之群.Cl_Cl°-烷基、Ci-Ci。-鹵代烷基、C3-C丨。-環烷 基、c3-c:10-南代環烷基、c3_Ci〇_環烷基曱基、鹵 代=烷基甲基、c2-Ci〇-烯基、C2-C10-鹵代烯基、Ci_d 烷乳基-CrCw燒基、笨基、节基、笨氧基-甲基、 貝雜方基、5-^6昼施笔且田甘 ++丄 次6員雜方基曱基,其中上述最後5個基團 133661.doc 200917962 中之(雜)芳香族環可未經取代或可具有卜2、3、4或玲 相同或不同取代基RX,其係選自#素、Cl-C4-烷基\ Ci_ C4-鹵代烷基、C|_c4-烷氧基、c,-c4-自代烷氧基、C|_ cv烷基磺醯基、及Ci_C4_鹵代烷基磺醯基。土 ' 31·如請求項1至7中任—項之方法,其中該等無脊椎害蟲係 節肢動物害蟲及/或線蟲。 32.如清求項31之方法,其中該等無脊椎害蟲係昆蟲。 ,33·如請求項32之方法,其中該等無脊椎害蟲係同翅目 (H〇moptera)昆蟲。 U項1至7中任-項之方法’其中該等無脊椎害蟲係 蜗蟲。 35. -種保護植物繁殖材料及/或自其生長之植物之方法,該 方法包含用殺蟲有效量之如請求項】至3〇中任一項所定 義之式I或II化合物或其農業上可接受之鹽或N_氧化物處 理該種子。 ( 36·帛植物繁殖材料,其包含至少一種如請求項上至3〇中 任-項所定義之式則化合物及/或其農業上可接受之鹽 或N-氧化物。 37. —種如請求項β30中任—項户斤定義之^或⑽合物或 其獸醫學上可接受之鹽或N_氧化物之用途,其用於製造 治療或保護動物免受寄生蟲侵擾或感染之藥物。 38. —種式I或π。比唑化合物 133661.doc •15- 200917962Mie and its bonded nitrogen atom form a 5 or 6 membered saturated or unsaturated heterocyclic ring 'which may have another hetero atom selected from fluorene as a ring member atom and wherein the heterocyclic ring may be unsubstituted or Having i, 2, 3, 4 or 5 substituents independently of one another selected from the group consisting of: a phytol, a cyano group, a nitro group, a Cl_C4 {yl group, an alkyl group, a CVCV alkoxy group, and a CVC^haloalkane氧基; R is selected from (VC4-alkyl, q-cv-alkyl, c3_C6_cycloalkyl, C3-C6-halocyclo, c2_c4_dilute, C2_C4_ _, dilute, C2- C4-alkynyl, CVC4-alkoxy-Ci_c4-alkyl, phenyl, heteroaryl, phenyl-CrC4-alkyl and heteroaryl·Ci_c4_alkyl, wherein the last four groups are aromatic The ring may be unsubstituted or may have 133661.doc 200917962 R8 R (Re 1, 2, 3, 4 or 5 are independently selected from each other consisting of: a base: a cyclin, a cyano group, a thiol group, a Ci oxime a group, a c-alkyl group, a Cl_C4_ alkoxy group, and a Ci_C4-sodium alkoxy group; the ~ groups are independently selected from the group consisting of hydrogen, Ci oxime, Ci_c^, alkyl, C3_C6_cycloalkyl, c3-c6 ·Circular base methyl, C"C6 self-generation ring burning Base, q-CV fluorenyl group, C2_C4•equivalent alkenyl group, c2_c: group, Cl-C4-alkoxy group _Cl oxime group, phenyl group, heteroaryl group: the group -C丨-(V alkyl group and a heteroaryl group, wherein the aromatic ring of the above four groups may be unsubstituted or may have i, 2, 3, 4 or 5 substituents independently of each other selected from the group consisting of dentate, cyanide a nitro group, a cyanoalkyl group, a Ci(R) group, a CVC4. alkoxy group, and a Ci_C4_haloalkoxy group; selected from the group consisting of CVC4-alkyl, C1 々 々 alkyl, C3_C6_cycloalkyl' C3-c6-cycloalkylmethyl, C3_C6 definite cycloalkyl, dilute, c2_c4_Southern alkenyl, C2_C4_alkynyl, Ci_c4_homolyl_ycv alkyl, stupyl, heteroaryl, benzene Based on ''alkyl and heteroaryl-Cl-C4_alkyl, wherein the aromatic ring of the last four groups described above may be unsubstituted or may have 1, 2, 3, 4 or 5 independently selected from each other Substituents of the group consisting of: γ, aryl, nitro, cvk, Ci_C4_haloalkyl, sulfoxy and Ci-C4-haloalkoxy; independently selected from each other Hydrogen, Ci_C4_alkyl, Ci_c4^, f, C3-C6-ring, C3_C6•cycloalkane Sulfhydryl, C3_C6_functional cycloalkyl, C2-(V alkenyl, C2_C4_ by alkenyl, c2 core-block 133661.doc 200917962, kcv morphoxy_Cl_C4), Ci_c4_alkyl , Cl-CV dentate alkylcarbonyl, c^c4-alkylsulfonyl, Ci_C4-dentate, aryl, phenyl, phenyl, phenylphenyl, heteroaromatic heteroaryl Carbonyl, heteroarylsulfonyl, phenyl_C|_C4_alkyl, heterocyclyl-CrCV alkyl group. The aromatic ring in the last 8 base circles described above may be unsubstituted or may have J, 2 , 3, 4 or 5 substituents independently of one another selected from the group consisting of dentate, cyano, nitro, CVCV alkyl, Cl_c4_descriptive, Ci_c4 methoxy and Ci-Cr haloalkoxy Or R and R and the nitrogen atom to which they are bonded form a 5- or 6-membered saturated or unsaturated t-heterocyclic ring which may have another hetero atom selected from the group consisting of fluorene, s &amp; N as a ring member atom and wherein the The ring may be unsubstituted or may have i, 2, 3, 4 or 5 substituents independently of one another selected from the group consisting of halogen, cyano, nitro, Cl_c4_alkyl, Ci_c alkyl, CrC4 ·Alkoxy and (^-(:4-haloalkane) Rg, Rh are independently selected from hydrogen, Cl_c4_alkyl, Ci_c4__alkyl, c3-c6-cycloalkyl, C3-C6-i cycloalkyl, c2_c44, C2-C4- Halogenated, C2-C4-blockyl, Cl_c4•院oxy_Cl-C4-alkyl, phenyl, heteroaryl, phenyl-(:1&lt;4-alkyl and heteroaryl-C^ -C4.alkyl, wherein the aromatic % of the last four groups described above may be unsubstituted or may have 1, 2, 3, 4 or 5 substituents independently of one another selected from the group consisting of: a cyano group, a nitro group, a CVC4-Huan group, (VC4-haloalkyl group, Cl-c4-alkoxy group, and C1-C4-halodecyloxy group; 133661.doc 200917962 R, selected from the group consisting of: A , Cl-c4-alkyl, Cl-C4 dentate alkyl, c3-c6-ring; 13⁄4, c3_c6 cycloalkyl, C3_C6_white, alkyl, C2-C4-, c2_c4_ _ a C2_C4_alkynyl group, a C1-C4_alkoxy-C丨-cv alkyl group, a phenyl group and a phenyl-Cl_4 alkyl group, wherein the benzene ring in the last two groups may be unsubstituted or may have 1, 2 '3, 4 or 5 substituents independently of each other selected from the group consisting of: halogen, cyano, nitro, Ci_c4_alkane a group, c^-c: 4-haloalkyl, Cl_C4_alkoxy and Ci_C4_haloalkane; Rx is selected from the group consisting of halogen, cyano, nitro, Cl_C4-alkyl, VC4-haloalkyl, CVC4-alkoxy, CVC4-haloalkoxy, (VC4-alkylthio, CVC4-haloalkylthio, C,-C4-alkyl sulphate, Ci-C4_halogenation) a genus, a C 1 -c4-alkylsulfonyl group, a Ci-Cr haloalkylsulfonyl group, a c,-c4-alkylcarbonyl group, a CVC 4-haloalkylcarbonyl group, a c3-c6-cycloalkyl group, C3-c6-halocycloalkyl, c2-c4-alkenyl, c2-c4-haloalkenyl, c2-c4-alkynyl and CVC4-alkoxy-CrCU-alkyl; Ry is independently selected from each other From C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-halooxy, C1-C4-sulfuryl, C1-C4-halogenated Sulfur-based, ci-c4-alkyl sulphate, Ci_C4_haloalkyl sulfhydryl, C1-C4_alkyl sulfhydryl, Cl_C4_haloalkylsulfonyl, C3-C6- Cycloalkyl, CVCe-halocycloalkyl, C2·C4-alkenyl, C2-C4-haloalkenyl, C2-C4-alkynyl, G-C4-alkoxy-CVC4-alkyl, and CVCn- Alkylcarbonyl. 133661.doc -9- 200917962 2. The method of claim 1, wherein the pyrazole compound is a compound of formula j. 3. The method of claim 1, wherein the pyrazole compound is a compound wherein X1 in formula I is oxygen. 4. The method of claim 1, wherein the pyrazole compound is a hydrazine compound, wherein R1 is hydrogen, CN, Cl-Cl0-alkyl, Cl-Cl〇-haloalkyl, c2·Cio-alkenyl, C2-C10-haloalkenyl, C2-C10-alkynyl, C^-CV alkoxy-Cl~cio-alkyl, CVC4-alkylene-CN, 〇Ra, C(Y)Rb, c( Y) 〇 Re or s(o) 2Rd. 5. The method of claim 4, wherein R is hydrogen, CrCV alkyl or Cl_c4_extension-CKf. 6. For example, π! A method wherein R2 is hydrogen, decyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy or trifluoromethoxy. 7: The method of claim, wherein r3 is hydrogen, methyl, difluoromethyl, tri-gas: methoxy, difluoromethoxy or trifluoromethoxy = &gt; The method of 6 or 7, wherein the groups are hydrogen. 4 夕1固 9 · The claim 8 $ t &amp; method, wherein the groups R2 and R3 are both hydrogen. 1〇_If the request item is 7 to η. If the request item ίο is the party* Γ is the group A1. , CN, 法, 中R4丨 and R51 are independently selected from hydrogen, tooth ', , Cl-C1G-mercapto, C, Γ « 广C2-C丨0-alkyne, 甘屮1〇-echane The aliphatic, 1 part of the last 4 groups of the above-mentioned C2-C-decenyl group and N8 may be unsuppressed by π Α Τ夂钿 禊 or % η ° 邛 or completely halogenated or may have} Biting two identical or different substituents Ry. A 2 phases 12 · as claimed in 丨 ', where R41 and R51 are independently selected from each other 133661.doc -10- 200917962 wind, CN, halogen, C丨-c4-alkyl, C丨-c4- _ generation Alkyl, c3_c decyl and C3_C6· _cycloalkyl. 13. The method of claim 12, wherein R41 and R51 are independently selected from the group consisting of hydrogen, CN, halogen, CH3, CH2f, CHf2, and cf3. 14. The method of claim 13, wherein R41 or R51 is hydrogen or both R41 and R51 are 15. The method of claim 10, wherein R61 is selected from the group consisting of: Cl ClG_alkyl, Dai Hyun , C3-C1G-cycloalkyl, c3_c10_halogenated alkyl, C3_C10-cycloalkylmethyl, C3-C10-halocycloalkylmethyl, c2-c10-alkenyl, c2-C10-dentate Alkenyl, CrCr alkoxy_Ci_c1〇-alkyl, phenyl, benzyl, phenoxy-fluorenyl, 5- or 6-membered heteroaryl, 5- or 6-membered heteroarylmethyl, wherein The (hetero)aromatic ring in the last 5 groups may be unsubstituted or may have an anthracene, 2, 3, 4 or 5 identical or different substituents RX selected from halogen, Ci_C4_alkyl, alkane a method of claim 15, wherein the method is the method of claim 15, wherein the method comprises the method of claim 15, wherein the method is the method of claim 15, wherein the method is the method of claim 15, wherein the method of claim 15 R6, is a method of any one of the preceding claims, wherein A is a group A2. 18. The method of claim 17, wherein the R42 is Selected from hydrogen, halogen, c4-hospital, Cl-c4 deuterated, C3_C]G_cycloalkyl, 匕_^__ a cycloalkyl group and a phenyl group which may be unsubstituted or may have an anthracene, 2, 3, 4 or 5 identical or different substituents V selected from the group consisting of halogen, Ci_C4 alkyl, CVCV haloalkyl, CVCV alkoxylate And //halohaloalkoxy. 133661.doc -11 - 200917962 19. The method of claim jg彳s 4 &amp; 8, wherein R42 is selected from the group consisting of hydrogen, halogen, CN 匕 4 · hospital base, Γ , 匕1-i-C4-haloalkyl, C3-C6-cycloalkyl and cc cycloalkyl. &quot;·sighing halogen 20·as requested jg〗 7 + + hydrogen, from ♦, R52 is selected from The following groups: ", CN, c] - cI0 - pit base, Cl_Cl " generation cc ^ C3_Cl 〇 - halocycloalkyl, c3-c10-cycloalkylmethyl, 3 cycloalkyl fluorenyl, C2 -CI()-alkenyl, ^yl-c]-c丨0-alkyl, phenyl, benzyl, phenoxy A_ T -3⁄4 ' AL· λ*- ** sulphate, 5- or 6-membered heteroarylmethyl, wherein the (hetero)aromatic ring in the upper, ten, and 2 groups may be unsubstituted or may have 1 appearance group 4 or: one: the same ^ C1-C4-resolution Alkyl, Ci_c4_alkoxy, h-c4-halo 1 c4-alkylindenyl, and Ci_ 21.沉基%醯基. Nitrogen, 1Γ' wherein R52 is selected from the group consisting of: leucovorin, TM, Cl_Cl. -alkyl, CH dentate, Cio-cycloalkyl, c Γ 占 k ((3- CC ^ halocycloalkyl, 4-(^- ring-based methyl, 3 10 ·'----- Methyl, c2-cI0-alkenyl, cc and Ci-C4-; Jt oxygen A p ^ 2-C1 (r卣 alkenyl hydrazide-Ci_C丨0-alkyl. 22. The method wherein r62 is selected from the group consisting of hydrogen, kc10, and CVC, and CVC is a group consisting of C3-C 1 Cl0-haloalkyl, C3-Cl0-cycloalkyl, c"i〇·self-generation ring, c"Ci0•环院基甲 alkylmethyl, C, C, method 1 c3-c丨0-_-cyclic group-CVC ^ Cl^ 归 、, Cl-C4_ oxynitride 1丨c丨〇- Alkyl, phenyl, oxime, benzyl, phenoxy and phenoxy fluorene can be unsubstituted or can be 133661.doc -12- 200917962 has 1 , 2, 3, 4 or 5 identical or different substituents RX selected from halogen, CVCV alkyl, (Vc4-haloalkyl, cvcv alkoxy, C1-C4-halogenated emulsifier, G-C4 - A sulphate base, and a Q-C4-halogenated p-based base. 23. The method of claim 22 wherein R62 is hydrogen, c丨-C4-alkyl or halodecyl. The method of any one of claims 1 to 7, wherein a is a group A3. 25. The method of claim 24, wherein R43 is selected from the group consisting of hydrogen, halogen, CN, r c4_alkyl, C丨-C4-haloalkyl, c3_Cl〇-cycloalkyl, c3_Ci〇_Southern cycloalkyl and phenyl which may be unsubstituted or may have 1 '2, 3, 4 or 5 identical or different substituents Rx, It is selected from the group consisting of halogen, Ci_C4_alkyl, CVC4-haloalkyl, CVC4-alkoxy, Cl_C4_haloalkoxy, C1-C4.alkylsulfonyl, and Ci-C*-haloalkylsulfonyl. 26. The method of claim 2, wherein r43 is selected from the group consisting of hydrogen, halogen, CN, c4-alkyl, CVC4-haloalkyl, c3_c6-cycloalkyl, and c3_c6•halocycloalkyl. The method wherein R53 is selected from the group consisting of hydrogen, halogen, CN, (:, -(:)-alkyl, (:,-(:]-haloalkyl' c3_ Ci〇-cycloalkyl 'C3-C10-halocycloalkyl, c3_C10-cycloalkylindenyl, c3-c丨0-halocycloalkylindenyl, C2_Ci〇•alkenyl, C2_Ci〇_ _alkenyl, Ci-cv Alkoxy _Cl-Cl (r alkyl, strepyl, benzyl, phenoxy fluorenyl, 5- or 6 a heteroaryl, 5- or 6-membered heteroarylmethyl group, wherein the (hetero)aromatic ring in the last five of the above groups may be unsubstituted or may have i, 2, 3, 4 or 5 identical or different Substituent RX, which is selected from the group consisting of halogen, 133661.doc -13· 200917962 c4-alkyl, CVC4-halogenyl, Cl_C4_alkoxy'c〗_c4-haloalkoxy, CVC4-alkylsulfonyl And the Cl_C4_ letter generation base. 28. The method of claim 27, wherein r53 is selected from the group consisting of hydrogen, halogen, CN, Ci-Cio-alkyl, Ci-C10_haloalkyl, 匸3_ Ci〇-ring, C3_Ci〇-halogenated cycloalkyl, C3_Ci〇-i alkyl, C3-C10-halocycloalkyl, C2-C10-dilute, C2-C10-halogenated or C 1 - C 4 -theoremium_C 1 -C 1 0 -alkyl. 29. The method of claim 24, wherein R63 is selected from the group consisting of: murine, Ci-Ci〇-alkyl, Ci-Ci〇-halogen, C3-C10-cycloalkyl, C3-C10 -halocycloalkyl, C3-C10-cycloalkylmethyl, C3-C10-halocycloalkyl, C2-Ci〇-dilute, C2-C10-halogenated, Ci-C4- ^oxy-CrC^o-alkyl, phenyl, benzyl, phenoxy-fluorenyl, 5- or 6-membered heteroaryl, 5- or 6-membered heteroarylmethyl, of which the last five The (hetero)aromatic ring in the group may be unsubstituted or may have 1, 2, 3, 4 or 5 identical or different substituents Rx ' selected from halogen, Cl_C4_alkyl, Ci_C4-acid Base, CVC 4-homoyloxy, Ci-C4-halo-oxyl, decyl-acid group, and Ci-C4-haloalkylsulfonyl. 30. The method of claim 29, wherein r53 or R63 is hydrogen, Ci_C4_alkyl or GC: 4-haloalkyl, and the other group of R53, R63 is selected from the group consisting of: - alkyl, Ci-Ci. - haloalkyl, C3-C丨. -cycloalkyl, c3-c: 10-s-cycloalkyl, c3_Ci〇-cycloalkylindenyl, halo=alkylmethyl, c2-Ci〇-alkenyl, C2-C10-haloalkenyl , Ci_d alkane-based, CrCw, base, stupid, stupidoxy-methyl, berylungyl, 5-^6昼, pen, and Tiangan++丄6, 6-membered hetero-based fluorenyl, Wherein the (hetero)aromatic ring in the last five groups 133661.doc 200917962 may be unsubstituted or may have the same or different substituent RX, which is selected from the group consisting of #素, Cl-. C4-alkyl\Ci_C4-haloalkyl, C|_c4-alkoxy, c,-c4-autoalkoxy, C|- cv alkylsulfonyl, and Ci_C4_haloalkylsulfonyl. The method of any one of claims 1 to 7, wherein the invertebrate pests are arthropod pests and/or nematodes. 32. The method of claim 31, wherein the invertebrate pest is an insect. The method of claim 32, wherein the invertebrate pest is a H. moptera insect. The method of any one of items 1 to 7 wherein the invertebrate pests are worms. 35. A method of protecting a plant propagation material and/or a plant grown therefrom, the method comprising using a pesticidally effective amount of a compound of formula I or II as defined in any one of claims 3 to 3 or agricultural The seed is treated with an acceptable salt or N-oxide. (36) A plant propagation material comprising at least one compound of the formula as defined in the claims to claim 3 and/or an agriculturally acceptable salt or N-oxide thereof. The use of any of the claims β30, or a pharmaceutically acceptable salt or N-oxide thereof, for the manufacture of a medicament for the treatment or protection of an animal from parasite infestation or infection 38. —Formula I or π.Biazole compound 133661.doc •15- 200917962 R1 R&quot; (0 其中 A、X1、X2、RR1 R&quot; (0 where A, X1, X2, R R及R3係如請求項丨中所定義 其鹽及N-氧化物’不包括符合以下條件之式〗化合物 -A具有式A2,X1為Ο,Ri、R2、R3、r42及r62各自為 氫,且R53為2-羥基苯基、2-羥基甲基苯基、孓羥 基-5-乙基苯基、2-羥基-5-氣苯基、2_羥基_4,5_二甲 基本基、2-¾基-3,4 - 一曱基苯基或2 -經基-3,5-二曱烏 苯基, -A具有式A3 ’ X為Ο ’ R1、R2、R3、R4 3及r6 3各自為 氫’且R53為苯基、4-氟苯基、4-甲氧基苯基、4-淳 苯基、4-氯苯基、4-甲基苯基、4-乙氧基苯基、2,4_ 二甲基苯基、2-羥基苯基、2-羥基甲基苯基、 經基-5-乙基苯基、2-經基-5-氯苯基、2-經基-4,5-二 甲基笨基、2-羥基-3,4-二甲基苯基或2-羥基-3,5-二甲 基苯基, -X1為0,R1、R2及R3各自為氫且A係1-(苯基曱基)-3-硝基吡唑-5-基、1-甲基吡唑-5-基、1-甲基-4-氯吡唑-5 -基、1-乙基-4-漠°比〇坐-3-基、1-乙基-3-甲基0比。坐-4_ 基、1-曱基-3-三氟曱基吡唑-4-基、1-苯基-5苯曱醯 基胺基吼唑-4-基、1-(4-氣苯基)-3-苯基胺基羰基-5-甲基吡唑-4-基、1-苯基-5-[(4-甲基苯基)羰基]胺基吼 唑·4-基、4-碘吡唑-3-基、1-甲基吡唑-3-基、5-氣-1- 133661.doc •16- 200917962 曱基吡唑-3-基、5-硝基吼唑-3-基、ι_(4_氣苯基)_5-二I甲基0比唾-4-基、1-苯基-3-嚯吩_2_基0比。坐·4-基、 1-苯基-3,5-二甲基吡唑-4-基、4-溴-5-琐基吡唑-3-基、5-%丙基_1_(1,1-二氧代四氫11塞吩-3_基)-11^-0比 唑-3-基; 且亦不包括以下化合物: &quot;1_(4·氣笨基)-5-三氟曱基-1Η-。比嗤_4-甲酸《»比咬-3-基 醯胺、 -丨-苯基-3-噻吩-2-基-1Η-吡唑-4-甲酸吡啶·3_基醯胺、 -3,5_二曱基-1-苯基-1Η-吼唑-4-甲酸〇比啶_3_基醯胺。 39_如請求項38之化合物,其具有式I。 40. 如請求項38之式I化合物,其中X1為氧。 41. 如請求項38之式j化合物,其中Ri係氫、Ci_Ci〇_烷基、 CN li_C10-鹵代炫基、c;2-Ci〇-稀基、c:2_c10_鹵代烯 基、C2-C1G-炔基、CVC4-烷氧基-CVCw烷基、C丨-C4-伸 烷基-CN、〇Ra、C(Y)Rb、C(Y)〇Rc^ s(〇)2Rd。 42. 如請求項41之化合物,其中Rl係氩、Ci_C3_烷基或匕心-伸烷基_CN。 43. 如請求項38之化合物,其中R2係氫、甲基、二氟曱基、 三氟甲基、甲氧基、二氟甲氧基或三氟甲氧基。 44. 如請求項38之化合物,其中R3係氫、曱基、二氟曱基、 二氣甲基、甲氧基、二氟甲氧基或三氟甲氧基。 45. 如請求項43或44之化合物,其中該等基團尺2或r3中至少 一個為氫。 133661.doc 17- 200917962 46. 如請求項45之化合物’其中基團R2及R3二者皆為氮。 47. 如請求項38至44之化合物,其中A為基團A1。 48·如請求項47之化合物,其中R41及R51係獨立地選自氧、 i 素、cn、Ci-Ci。-烧基、c3-c1Q-環院基、c2_Ci()_歸久 及C2_C10-快基,其中上述最後4個基團中之脂肪族或環 狀部分可未經取代、可部分或完全^化或可具有1或2個 相同或不同取代基Ry。 49. 如請求項48之化合物,其中^丨及尺5丨係彼此獨立地選自 氫、鹵素、CN、C〗-C4-烷基、CVC4-鹵代烷基、C3_C6_ 環烷基及C3-C6-鹵代環烷基。 50. 如請求項49之化合物,其中R41及R”係彼此獨立地選自 氫、鹵素、CN、CH3、CH2F、CHF2&amp;CF3。 51. 如請求項50之化合物,其中r414R5i為氫或R4i及rS1二者 皆為氨。 52_如請求項47之化合物,其中R6!係選自由以下組成之群: ci-c10-烷基、c,-c10-函代烷基、c3-c10-環烷基、C3_Ci。-齒代環烷基、(VC10-環烷基甲基、C3_Ci〇_鹵代環烷基^ 基 C2-C10-烯基、C2-Ci〇-鹵代稀基、c^-Cf院氧基 烷基、苯基、节基、苯氧基_甲基、5_或6員雜芳 基、5-或6員雜芳基曱基’其中上述最後5個基團中之 (雜)芳香族環可未經取代或可具有1、2、3、4或5個相同 或不同取代基Rx,其係選自鹵素、Ci_C4_烷基、卤 代烷基、C^CV烷氧基、CVC4·鹵代烷氧基、Cl_c4_烷基 石黃酿基及Ci-C4-鹵代烷基磺醢基。 133661.doc •18· 200917962 53·如請求項52之化合物,其中R0丨係Ci_C4_烷基或c〗_c4__ 代烷基。 5 4 ’如明求項3 8至44之化合物,其中A係基團A2。 %如請求項54之化合物,其中r42係選自氫、南素、cn、 Ci-c4道基、Cl_c4_ _ 代燒基、C3_C]G 说 名 四 ^10- 厂環烷基及苯基,其可未經取代或可具有丨、2、3、4 或5個相同或不同取代基RX ’其係選自齒素、c】_c4-燒 基、h-cv鹵代院基、c]々烧氧基、Ci々齒代烧氧 基' Ci-Cc烷基磺醯基、及Ci_C4_鹵代烷基磺醯基。 56. 如請求項55之化合物,其中r42係選自氫、㈣、⑶、 CVCV烷基、Cl_c4-鹵代焓其、Γ Γ 甘 代環貌基。 代坑基W㈣基及C3-CV幽 57. ^月求項54之化合*,其中r52係選自由以下組成之群: =、,素、CN、Cl-ClQ-烧基、C〗-C1(r _ 代烧基、c _ V 烷基、C3_c“代環烷基、Μ。·環烷基甲基: 基c=代環烧基甲基、c2-ClQ_烯基、c2_Ci。嗰代烯 1 4_烷乳基烷基、笨基、节基、苯氧 :基、5·或6員雜芳基、5_或6員雜芳基甲基 : 最後5個基團中r雜 ’、中上迷 中之(雜)方香族環可未經取代或可具U、 、、:或5個相同或不同取代基RX,其係選自画 C4-院基、CVC4代燒基、Ci_C4_貌氧基、 「 烷氧基、Ci々烷基磺醯基 =1 4-自代 58. 如請求項54之化合物,其中二二。广烧基續酿基。 氫、C丨-Cl_俨其„ 自由以下組成之群: ° 70 &quot; '广^0· _代烷基、C3-C丨〇-環烷基、 133661.doc -19· 200917962 c3-c10-鹵代環烧基、c3-C10-環烧基甲基、c3-c10-鹵代環 烧基甲基、C2-C10-烯基、C2-C10-鹵代烯基、Ci-Cr烷氧 基烷基、苯基、5員雜芳基、苄基及苯氧基甲 基’其中上述最後4個基團之芳香族環可未經取代或可 具有1、2、3、4或5個相同或不同取代基Rx,其係選自 函素、cvcv烷基、(VCV鹵代烷基、cvcv烷氧基、 Ci-C4_鹵代烷氧基、q-C4-烷基磺醯基、及CVC4-鹵代燒 基磺醯基。 59. 如請求項58之化合物,其中r62係氫、Ci_c烷基、 11 _ C4 _代烧基、c3-C6 -環烧基或C3-C6-南代環烧基。 60. 如請求項44之化合物,其中a為基團A3。 61. 如請求項6〇之化合物,其中r43係選自氫、鹵素、CN、 Ci-C4-烷基、crC4-鹵代烷基、C3-C10-環烷基、c3-c 齒代環烷基及苯基’其可未經取代或可具有1、2、3、4 或5個相同或不同取代基Rx,其係選自鹵素、C]_C4、燒 基 C1-C4-鹵代烧基、(3^-C4 -炫氧基、C1-C4-鹵代燒氣 C1 C4-烧基石頁酿基、及鹵代烧基續酿基。 62. 如請求項61之化合物,其中R43係選自氫、鹵素、CN、 Cl_C4-燒基、C丨_c4-鹵代燒基、C3-C6-環烷基及c3_c太 代環烷基。 63·如清求項60之化合物,其中R53係選自由以下組成之群· 風、南素、CN、CVC,。烷基、(:丨-(:10-鹵代烷基、 ^ 3 - 1〇-環燒基、c3-c10-卣代環烷基、c3-c10-環烷基曱基、 C3_CW _代環烷基曱基、C2_Cl0_烯基、C2_Ci〇_ _代缔 133661.doc •20- 200917962 甲基 ” 員雜方基、5_或6員雜芳基甲基,其中上述 取後5個基團中之(雜)芳香族環可未經取代或可具有1、 2、3、4或5個相同或不同取代基rx,其係選自齒素、。_ c4-燒基、c丨-C4-鹵代桉其 ^ ^ 院氧A丨々院氧基、Cl々齒代 64 基續醯基、及㈣-自代炫基俩基。 。之化合物’其中R63係選自由以下组成之群: !:烷基、。夂“代烷基、Μι。·環烷基、 ^七】〇-_代環院基、 _ ^ ^ ^ ^ 烧基甲基、eve M ~Cl°·齒代環 A c 2 10、 土、C2_Cl〇-鹵代烯基、C丨-C4_烷氧 基-C丨-Ct烷基、苯基、苄基、 乳 芳基、5-或6員雜芳r甲基、5-或6員雜 (#)^ # ^ ' 土 土,其中上述最後5個基團中之 (雜)方香族環可未經取代 或不同取代基有&quot;。,個相同 代烷基、c,-c4-烷氧基、 1 4'* w )-cv鹵代烷氧基、CrCV、# A 崎醯基、及c,-c4m基續醯基。 4坑基 A如請求項Μ之化合物,其巾r53或 烧基或…代院基,同時R53、R63之】CN、C&lt; 由以下組成之群:C|_c 基團係選自 C,。-環烷基、c3C “…、Cl-Cl°'南代烷基、C3-h-c丨0-齒代環烷基、C3_c C3-C“代環烷基甲基 h 土甲基、 12 基、ρ ρ 基、kcv院氧基_Ci_Ci〇道基、苯基、节=代晞 =基、5-或6員雜芳基、5_“員雜芳基土本乳基- 最後5個基團中之 土,其中上述 中之(雜)-香族環可未經取代或可具有卜 133661.doc -21 . 200917962 2、3、4或5個相間+ τ J或不同取代基Rx,其係選自鹵素、C,- c4-烷基、cvc4-鹵代烷基、Ci_C4_烷氧基、Ci_C4_鹵代 炫1氧基Ci-C4_烧基績醯基、及Ci_C4_鹵代烧基績酿基, 其中R53亦可為鹵素。 66· —種農業組合物,其含有至少—種如請求項38至65中任 一項所定義之式I或Π化合物及/或其農業上可接受之鹽或 N-氧化物及至少一種液體或固體载劑。 133661.doc 22- 200917962 七、指定代表圖: (一) 本案指定代表圖為:(無) (二) 本代表圖之元件符號簡單說明: 八、本案若有化學式時,請揭示最能顯示發明特徵的化學式:R and R3 are as defined in the claims, and the salts and N-oxides do not include the formula: - A has the formula A2, X1 is hydrazine, and Ri, R2, R3, r42 and r62 are each hydrogen. And R53 is 2-hydroxyphenyl, 2-hydroxymethylphenyl, oxime hydroxy-5-ethylphenyl, 2-hydroxy-5-phenylphenyl, 2-hydroxy- 4,5-dimethyl basic , 2-3⁄4 base-3,4-mercaptophenyl or 2-butyryl-3,5-diindenylphenyl, -A has the formula A3 'X is Ο 'R1, R2, R3, R4 3 and R6 3 is each hydrogen ' and R53 is phenyl, 4-fluorophenyl, 4-methoxyphenyl, 4-anthracenephenyl, 4-chlorophenyl, 4-methylphenyl, 4-ethoxyl Phenyl, 2,4-dimethylphenyl, 2-hydroxyphenyl, 2-hydroxymethylphenyl, benzyl-5-ethylphenyl, 2-yl-5-chlorophenyl, 2- -4,5-dimethylphenyl, 2-hydroxy-3,4-dimethylphenyl or 2-hydroxy-3,5-dimethylphenyl, -X1 is 0, R1, R2 and R3 Each is hydrogen and A is 1-(phenylindenyl)-3-nitropyrazol-5-yl, 1-methylpyrazol-5-yl, 1-methyl-4-chloropyrazole-5- The base, 1-ethyl-4-indol is higher than the -3-yl, 1-ethyl-3-methyl 0 ratio. -4-yl, 1-mercapto-3-trifluoromethylpyrazol-4-yl, 1-phenyl-5phenylnonylaminocarbazole-4-yl, 1-(4-phenylphenyl --3-phenylaminocarbonyl-5-methylpyrazol-4-yl, 1-phenyl-5-[(4-methylphenyl)carbonyl]aminocarbazole-4-yl, 4- Iopyrazole-3-yl, 1-methylpyrazol-3-yl, 5-gas-1-133661.doc •16- 200917962 decylpyrazol-3-yl, 5-nitrocarbazole-3- Base, ι_(4_gasphenyl)_5-di-Imethyl 0 is more than sp-4-yl, 1-phenyl-3-porphin-2-yl. Sodium 4-yl, 1-phenyl-3,5-dimethylpyrazol-4-yl, 4-bromo-5-zinopyrazol-3-yl, 5-%propyl_1_(1, 1-Dioxotetrahydro 11-cepan-3-yl)-11^-0-pyrazol-3-yl; and does not include the following compounds: &quot;1_(4·气笨基)-5-Trifluoromethane Base-1Η-.嗤_4-carboxylic acid "» than bit-3-yl decylamine, - fluorenyl-phenyl-3-thiophen-2-yl-1 Η-pyrazole-4-carboxylic acid pyridine · 3 - decylamine, -3, 5_Dimercapto-1-phenyl-1 oxime-oxazole-4-carboxylic acid guanidinium _3_ decylamine. 39. A compound of claim 38 which has the formula I. 40. A compound of formula I according to claim 38, wherein X1 is oxygen. 41. The compound of formula j of claim 38, wherein Ri is hydrogen, Ci_Ci〇-alkyl, CN li_C10-halothylenyl, c; 2-Ci〇-dilute, c:2_c10_haloalkenyl, C2 -C1G-alkynyl, CVC4-alkoxy-CVCw alkyl, C丨-C4-alkylene-CN, 〇Ra, C(Y)Rb, C(Y)〇Rc^s(〇)2Rd. 42. The compound of claim 41, wherein R1 is argon, Ci_C3_alkyl or fluorene-alkyl-CN. 43. The compound of claim 38, wherein R2 is hydrogen, methyl, difluorodecyl, trifluoromethyl, methoxy, difluoromethoxy or trifluoromethoxy. 44. The compound of claim 38, wherein R3 is hydrogen, decyl, difluorodecyl, di-methylmethyl, methoxy, difluoromethoxy or trifluoromethoxy. 45. The compound of claim 43 or 44, wherein at least one of the groups 2 or r3 is hydrogen. 133661.doc 17- 200917962 46. The compound of claim 45 wherein both the groups R2 and R3 are nitrogen. 47. The compound of claim 38 to 44, wherein A is a group A1. 48. The compound of claim 47, wherein R41 and R51 are independently selected from the group consisting of oxygen, i, cn, Ci-Ci. - an alkyl group, a c3-c1Q-ring group, a c2_Ci()_returned and a C2_C10-fast group, wherein the aliphatic or cyclic moiety of the last four groups described above may be unsubstituted, partially or completely Or it may have 1 or 2 identical or different substituents Ry. 49. The compound of claim 48, wherein the oxime and the ruthenium 5 are independently selected from the group consisting of hydrogen, halogen, CN, C-C4-alkyl, CVC4-haloalkyl, C3_C6_cycloalkyl, and C3-C6- Halogenated cycloalkyl. 50. The compound of claim 49, wherein R41 and R" are independently of each other selected from the group consisting of hydrogen, halogen, CN, CH3, CH2F, CHF2 & CF3. 51. The compound of claim 50, wherein r414R5i is hydrogen or R4i and rS1 is both ammonia. 52. The compound of claim 47, wherein R6! is selected from the group consisting of: ci-c10-alkyl, c, -c10-functional alkyl, c3-c10-cycloalkane Base, C3_Ci.-dentate cycloalkyl, (VC10-cycloalkylmethyl, C3_Ci〇_halocycloalkyl) C2-C10-alkenyl, C2-Ci〇-halogenated, c^- Cf oxyalkyl, phenyl, benzyl, phenoxy-methyl, 5- or 6-membered heteroaryl, 5- or 6-membered heteroaryl fluorenyl' among the last five of the above ( The heteroaromatic ring may be unsubstituted or may have 1, 2, 3, 4 or 5 identical or different substituents Rx selected from halogen, Ci_C4_alkyl, haloalkyl, C^CV alkoxy, CVC4·haloalkoxy, Cl_c4_alkyl sulphate and Ci-C4-haloalkylsulfonyl. 133661.doc •18· 200917962 53. The compound of claim 52, wherein R0 is a Ci_C4_alkyl or c __c4__ Alkenyl. 5 4 'If the item is 3 8 A compound of 44, wherein the A group A2. % is a compound of claim 54, wherein r42 is selected from the group consisting of hydrogen, nitrite, cn, Ci-c4, cyclyl, Cl_c4_ _, and C3_C]G ^10- Cycloalkyl and phenyl, which may be unsubstituted or may have hydrazine, 2, 3, 4 or 5 identical or different substituents RX' which is selected from the group consisting of dentate, c]-c4-alkyl, H-cv halo-based, c] anthracene oxy, Ci dentate alkoxy-Ci-Cc alkylsulfonyl, and Ci_C4_haloalkylsulfonyl. 56. The compound of claim 55, Wherein r42 is selected from the group consisting of hydrogen, (4), (3), CVCV alkyl, Cl_c4-halo oxime, Γ 甘 甘 环 。 。 。 代 。 代 代 代 代 代 代 代 代 代 代 代 代 代 代 代 代 代 代 代 代 代 代 代 代 代R52 is selected from the group consisting of: =, 素, CN, Cl-ClQ-alkyl, C--C1 (r _ alkyl, c _ V alkyl, C3_c "cycloalkyl, oxime." Cycloalkylmethyl: group c = cycloalkylalkyl, c2-ClQ-alkenyl, c2_Ci. decene 1 4 alkyl lactyl, stupid, benzyl, phenoxy: yl, 5· Or 6-membered heteroaryl, 5 or 6-membered heteroarylmethyl: the last 5 groups of r--, middle and upper fans The (hetero) aromatic ring may be unsubstituted or may have U, , or: or 5 identical or different substituents RX, which are selected from the group consisting of C4-yard, CVC 4 alkyl, Ci_C4_morphyloxy , "Alkoxy, Ci 々 alkyl sulfonyl =1 4-Self 58. The compound of claim 54, wherein two or two. Widely burned base continued to brew. Hydrogen, C丨-Cl_俨, „ Free group of the following: ° 70 &quot; '广^0· _ alkyl, C3-C丨〇-cycloalkyl, 133661.doc -19· 200917962 c3-c10 -halocycloalkyl, c3-C10-cycloalkylmethyl, c3-c10-halocycloalkylmethyl, C2-C10-alkenyl, C2-C10-haloalkenyl, Ci-Cr alkoxy Alkyl, phenyl, 5-membered heteroaryl, benzyl and phenoxymethyl' wherein the aromatic ring of the last four groups described above may be unsubstituted or may have 1, 2, 3, 4 or 5 The same or different substituent Rx, which is selected from the group consisting of a phytosin, a cvcv alkyl group, a (VCV haloalkyl group, a cvcv alkoxy group, a Ci-C4_haloalkoxy group, a q-C4-alkylsulfonyl group, and a CVC4-halogen 59. A compound according to claim 58 wherein r62 is hydrogen, Ci_c alkyl, 11 _C4 _ alkyl, c3-C6-cycloalkyl or C3-C6-s. 60. The compound of claim 44, wherein a is a group A3. 61. The compound of claim 6 wherein r43 is selected from the group consisting of hydrogen, halogen, CN, Ci-C4-alkyl, crC4-haloalkyl, C3-C10-cycloalkyl, c3-c dentate cycloalkyl and phenyl' which may be unsubstituted or may have 1, 2 , 3, 4 or 5 identical or different substituents Rx selected from halogen, C]-C4, alkyl C1-C4-haloalkyl, (3^-C4-methoxy), C1-C4-halogen A gas-fired C1 C4-alkyl sulphate base and a halogenated sinter base. 62. The compound of claim 61, wherein R43 is selected from the group consisting of hydrogen, halogen, CN, Cl_C4-alkyl, C丨_c4 a halogenated alkyl group, a C3-C6-cycloalkyl group, and a c3_c teraalkylene group. 63. The compound of claim 60, wherein the R53 is selected from the group consisting of: wind, south, CN, CVC, Alkyl, (: 丨-(: 10-haloalkyl, ^ 3 - 1 fluorene-cycloalkyl, c3-c10-decylcycloalkyl, c3-c10-cycloalkylindolyl, C3_CW _cycloalkane Base group, C2_Cl0_alkenyl, C2_Ci〇__代代133661.doc •20- 200917962 methyl" heteroaryl group, 5 or 6 membered heteroarylmethyl group, of which 5 groups are taken from the above The (hetero)aromatic ring may be unsubstituted or may have 1, 2, 3, 4 or 5 identical or different substituents rx selected from the group consisting of dentate, _c4-alkyl, c丨-C4- Halogenated 桉^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^ . The compounds' wherein R63 selected from the group consisting of the group consisting of:!: Alkyl,.夂"Alkenyl, Μι.·cycloalkyl, ^7] 〇-_ ring ring base, _ ^ ^ ^ ^ alkyl group, eve M ~ Cl ° · tooth ring A c 2 10, soil, C2_Cl〇-haloalkenyl, C丨-C4_alkoxy-C丨-Ct alkyl, phenyl, benzyl, arylaryl, 5- or 6-membered heteroaryl r-methyl, 5- or 6-membered Miscellaneous (#)^ # ^ ' soil, wherein the (hetero) aromatic ring in the last five groups above may be unsubstituted or different substituents have the same alkyl, c, -c4 - alkoxy, 1 4'* w )-cv haloalkoxy, CrCV, # A 醯 醯, and c, -c4m 醯 醯 4. 4 pit base A as claimed in the compound, its towel r53 or Burning base or ... substitute base, while R53, R63] CN, C&lt; group consisting of: C|_c group is selected from C, -cycloalkyl, c3C "..., Cl-Cl ° 'South Alkenyl, C3-hc丨0-dentate cycloalkyl, C3_c C3-C "cycloalkylmethyl h-m-methyl, 12-base, ρ ρ-group, kcv-oxo-Ci_Ci-ruthenium, benzene Base, knot = 晞 = base, 5- or 6-membered heteroaryl, 5_" heteroaryl aryl base - the soil of the last 5 groups, wherein the above (hetero)-fragrance ring Unsubstituted or may have 133661.doc -21 . 200917962 2, 3, 4 or 5 interphase + τ J or different substituent Rx selected from halogen, C, - c4-alkyl, cvc4-haloalkyl , Ci_C4_alkoxy, Ci_C4_haloxanoxy, Ci-C4_alkyl, and Ci_C4_haloalkyl, wherein R53 may also be halogen. 66. An agricultural composition comprising at least one of Formula I or a hydrazine compound as defined in any one of claims 38 to 65 and/or an agriculturally acceptable salt or N-oxide thereof and at least one liquid Or a solid carrier. 133661.doc 22- 200917962 VII. Designated representative map: (1) The representative representative of the case is: (none) (2) The symbol of the symbol of the representative figure is simple: 8. If there is a chemical formula in this case, please reveal the best display invention. Characteristic chemical formula: 133661.doc -6 ·133661.doc -6 ·
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